National Symposium on INTERFACING CHEMICAL …signpostejournals.com/ejournals/Portals/3/article_Brahmachari19.pdf · Recent past have witnessed the new infections and outburst of

Devdutt Chaturvedi,* Parmesh K. Dwivedi, Pragyandip P. Dash, Richa Srivastava (2015) Signpost Open Access J. Org. Biomol. Chem., 3, 142 - 284. Volume 03, Article ID 010323, 143 pages. ISSN: 2321- 4163 http://signpostejournals.com

142

National Symposium on

INTERFACING CHEMICAL BIOLOGY & DRUG DESIGN

(ICBDD 2015)

24-25 FEBRUARY, 2015

Convener

Dr. Devdutt Chaturvedi

Amity Institute of Pharmacy, Amity, Lucknow, UP, India

E-mail: [email protected]


143

Messages

Prof. (Dr.) Qamar Rahman, Ph.D, D.Sc (hc), FNASc, FST

Visiting Professor, University of Rostock, Germany

Adjunct Professor Hamdard University Delhi

Distinguished Professor, Amity University Noida Campus

Director & Dean Research (Science and Technology)

Amity University, Lucknow, India


Mobile: +91 9335229466

Message

Its a pleasure to congratulate, Amity Institute of Pharmacy, Amity University Uttar Pradesh,

Lucknow Campus, Lucknow, for organizing a two day National Symposium on the 24th and 25th

of February 2015 on “Interfacing Chemical Biology and Drug Design”.

One of the most significant contributions of synthetic organic chemistry is the improvement of

human health through the generation of biologically active compounds and pharmaceuticals.

In the 21st century emerging methods of diversity-oriented synthesis is poised to revolutionize the

discovery and development of new pharmaceuticals. Arising from the intersection of chemistry

and biology, these diversity-oriented methodologies combines the structural diversity of natural

products with the transformative power of synthetic chemistry to rapidly interrogate larger

expanses of biologically active chemical space than ever before possible.

I wish them success in their venture. I am sure that such symposiums will help to educate our

young pharmacists in their approaches.

mailto:[email protected]


144

Prof. (Dr.) M. V. Ramana,

Director, Amity Institute of Pharmacy

&

Chairman ICBDD 2015

Message

With accelerating growth in technology, the geographical demarcations ate continuously

constricting. World is engaged in drawing novel global boundaries of comprehensions. Hence, It

is a matter of great pride for me that Amity Institute of Pharmacy, Amity University Uttar Pradesh,

Lucknow Campus is organizing a national symposium on “Interfacing Chemical Biology and

Drug Design (ICBDD)”, which will provide a platform to the scholars and people from

pharmaceutical as well as chemical industries to discuss various perspectives of these two

interesting as well as simultaneously challenging spheres of science.

I wish that this multidimensional and intricate discussion would help the students and scholars to

acquire value based intellectual growth. I take this opportunity to applaud the convenor, organizing

secretary and all members of the steering committee for this initiative.

On behalf of the organizers and on my personal behalf, I wish the delegates a pleasant stay and

happy deliberating at ICBDD-2015.


145

Message

Amity Institute of Pharmacy acknowledges with gratefulness the concern, engrossment & the

earnestness with which the Pro Vice- Chancellor Maj. Gen K.K. Ohri and Dy. D. G. (Academics)

Prof. V. P. Sahi AUUP Lucknow Campus have supported the event. We are grateful to Amity

University Management for their continuous support for organization and conduction of Seminar

of National repute Second time in a row.

Recent past have witnessed the new infections and outburst of the old one including H1N1.

The theme of National Symposium on Interfacing Chemical Biology & Drug Design is very

appropriate and farsighted. I hope seminar will provide a common platform for research students,

academicians, researcher, pharmaceutical scientist and budding pharmacist to share their

knowledge and experience.

I believe that the souvenir will prove to be an effective instrument to present the vision of

the seminar and will be successful in achieving its objectives.

On behalf of organizing committee, I welcome all the dignitaries, speakers, delegates, advisors

and students for participating and encouraging us to make the event fruitful.

Dr. Sajal Srivastava

M. Pharm., Ph. D.


146

Dy. Director & Head

Amity Institute of Pharmacy

AUUP, Lucknow Campus

Message

Drug discovery process is an ultimate need for human beings for improvements and saving the

quality of life. Need of potent molecules for the treatment of various diseases such as cancer,

malaria, diabetes, inflammation, tuberculosis, HIV, CNS/CVS, and microbial infections etc. are

highly desirable nowadays. Marketed drugs of the respective diseases are directly/indirectly are

not much efficient or showing side effects. Therefore, need of drug developments to improve the

quality of life is highly desirable. The average overall cost of bringing a drug market is in excess

of 100 million dollars and the developmental time frame can be decade or longer. There is roughly

a 1 in 10,000 chance of a compound achieving the arduous trek from the laboratory to the market

place. The basic research aspects (synthetic-medicinal chemistry, pharmacology, molecular

biology etc.) of drug discovery may occur within the context of academic institutions, government-

sponsored agencies or the pharmaceutical industry. However, for all the practical purposes, the

costly and lengthy enterprise of developing an active lead compound to a marketed drug can be

most efficiently achieved by pharmaceutical companies which command the necessary financial

and interdisciplinary manpower. In recent years, in search for more potent drug molecules for a

particular disease, much progress has been made by the researchers around the globe, thus made

significant efforts in designing, synthesis and biological activities of plethora’s of series of

molecules.

The focus of the present symposium entitled National Symposium on “Interfacing

Chemical Biology and Drug Design (ICBDD-2015)” is to bring up a platform for knowledge

sharing experience in various areas of drug discovery and process research with emerging trends

and innovative techniques from the researchers of various academic/industrial institutions of India.

On behalf of organizing committee, I welcome all the dignitaries, speakers, delegates, advisors

and students for participating and encouraging us to make the event fruitful.


147

Dr. Devdutt Chaturvedi, Ph. D., PDF (USA & Germany)

Convener-ICBDD 2015

Amity Institute of Pharmacy

DRUGS AND THEIR USES

Person suffering from allergy can take chlorpheniramine,

To treat viral infections remember the use of acyclovir and rimantadine;

Methohexital is primarily used to induce anesthesia,

Paracetamol and other NSAIDs are famous to achieve analgesia;

Pentamidine is a drug for leishmaniasis,

Don’t forget the use of metronidazole to treat amoebiasis;

For treatment of epilepsy, phenytoin is perfect,

Lidocaine gives the local anesthetic effect;

Propanolol and nifedipine are used for hypertension,

Benzodiazepines can cause CNS depression;

An anti-bacterial is chloramphenicol,

The combination contraceptive is norethisterone and ethinylestradiol;

Drugs used for peptic ulcer are ranitidine and omeprazole,

Various fungal infections are treated with amphotericin B and fluconazole;

Adrenaline is a drug of choice in anaphylactic shock,

Atropine is useful in bradycardia and also in treating heart block;

Parmesh K. Dwivedi

(Treasurer)

ICBDD-2015


148

National Symposium on “INTERFACING CHEMICAL BIOLOGY & DRUG

DESIGN (ICBDD)”24-25 FEB. 2015

ORGANISING COMMITTEE

Chief Patron

Mr. Aseem Chauhan

Chancellor, Amity University Rajasthan

Chairman, Amity University Uttar Pradesh,

Lucknow Campus.

Patrons

Maj Gen K. K. Ohri, AVSM(Retd.)

Pro-Vice Chancellor,

Amity University Uttar Pradesh, Lucknow Campus

Prof. (Dr.) Q. Rahman,

Dean Research (S&T)

Amity University Uttar Pradesh, Lucknow Campus.

Prof. V.P. Sahi

Director, Amity Business School,


Chairman

Prof. (Dr.) M.V. Ramana

Director, Amity Institute of Pharmacy,



149

Convenor


Treasurers

Mr. Parmesh K. Dwivedi

Mr. Pragyandip Parthasarthi Dash

Ms. Richa Srivastava

Members:


Dr. Zeeshan Fatima

Ms. Mohini Chaurasia

Ms. Neha Mathur

Ms. Nimisha

Ms. Dipti Srivastava

Mr. Prakash Deep

Dr. Rahul Shukla

Mr. Saikat Sarkar

Mr. Amrit Kumar Singh

Ms. Suchita Dubey

Dr.Himani Awasthi

Mr. Nitin Srivastva

Ms. Sadaf Zaidi


150

STEERING COMMITTEE FOR ICBDD-2015

Sr.

No.

Committee

Name

Faculty Incharge/co-

incharge

Responsibility

1. Overall

Coordinator


1. Co-ordination with all the working

committees 2. Smooth

conduct of the event.

2. Marketing

ALL FACULTY OF

AIP.

1.To contact various agencies including

Banks, Publishers etc. for sponsorship and

follow-up

2.To contact various educational institutes

for registration of students in seminar

3. For Invitation

Dr.MV Ramana

Dr.Sajal Srivastava

Dr.Devdutt Chaturvedi

Ms.Sadaf Zaidi


1. Inviting dignitaries and guests for

Inaugural and Valedictory

2. Follow up of invites.

3. Coordinate with Transport committee

for the movement of invited local guests

and dignitaries

4. Hospitality

Mr. Pragyandeep Dash

Mr. Prakash Deep

Ms.Suchita Dubey

Mr. Parmesh Dwivedi

1. To decide Venue and Menu for

delegates. 2. Coordination

with Capt. Deepak Gandhi for Tea, lunch

and dinner.

3. Proper management of venue


151

5 MC(Master

Mr.Saikat Sarkar


1. Management of all the sessions

2. Collection and compilation CV and

topics of VIP’s, 3. Dignitaries & Guest

Speakers.

6 Transport

Ms. Neha Mathur

Mr. Pragyandip Dash

Dr. Rahul Shukla

1. Coordination & Escorting VIP & guest

speakers (Airport).

2. Maintaining travel plan of all the guests

3. Maintaining record of all the vehicles

(University Vehicle/Taxies)

4. Taking care of travel reimbursement of

guest speakers.

7. Hall

Management

Ms. Nimisha


Ms. Suchita Dubey

Mr. Saikat Sarkar


Mr. Parmesh

K.Dwivedi

1. Seating arrangement for Chief Guest,

Guest of honour and other invited

dignitaries and guest speakers.2. Display

of placards for seating plan for faculty,

speakers, delegates, students, press &

media etc.

3. Arrangement of mikes and other

requirements for PPT presentations

4. Decoration of hall, arrangement of

bouquet and citation etc.5. Coordination of

Inaugural ceremony & Valedictory

8. Disciplinary

Mr. Rahul Shukla

Mr. Pragyandip Dash

Mr.Parmesh K.

Dwivedi


Ms. Neha Mathur

1. Maintenance of proper discipline

outside and inside the auditorium both the

days.

2. To manage movement of students in and

out of Auditorium during sessions.3. Noise

control in the auditorium and auditorium

basement.

9.

Reception

Registration

And Certificate

Ms. Mohini Chaurasia

Ms.Richa Srivastava

Ms.Sadaf Zaidi

Dr.Himani

Ms.Nimisha

1. On-spot registration of delegates and

students.

2. Proper Maintenance of record of

registered students (Bank Draft)

3. Distribution of kits & Maintenance of

proper record.


152

4. Taking record of all participants (in

coordination with registration desk) and

the winners

10. Accommodation



Ms. Neha Mathur

1. Managing accommodation for guests

and delegates/students

2. Maintenance of record of guests &

delegates/students opted for

accommodation.

3. Preparation of chart for check-in &

Check out of guests.

11. Poster Display

Mr.Amrit Kr Singh

Dr. Zeeshan Fatima

Mr. Nitin Srivastava

1. Proper display of posters

2.Providing material for poster display

3. Coordination with judges

4. Compilation of results and handing over

results to certificate committee

12.

Report

compilation

Printing ,

Publishing

Media & Press


Dr.M.V.Ramana

Ms.Sadaf Zaidi

Mr. Ashutosh Chaubey

1. Designing, printing of Back drop and

Side drop and standees.

2. Printing of certificates

3. Inviting media persons and Follow up

4. Ensuring media coverage in all leading

English, Hindi & Urdu leading News

paper.

5. Providing press release

13.

Abstract

Screening &

Printing

Dr.MV Ramana

Dr.Sajal Srivastava

Dr.Devdutt Chaturvedi

Ms.Mohini Chaurasia

Mr.Parmesh Dwivedi

Ms.Richa Srivastava

Mr. Pragyandip Dash

1.To ensure screening of abstract and its

printing in a abstract book/CD


153

National Symposium on “Interfacing Chemical Biology and Drug

Design (ICBDD), 24-25th Feb. 2015

List of The Various Technical Sessions:

Day 1 (24/02/2014)

S.No Name of Activity Time Details of Activity 1. Registration of delegates 8:00 am onwards

2. Inaugural function 9:30 -9:40 am

9:40-9:50am

9:50-10:00am

10.00-10:10am

Lighting of lamp

Saraswati Vandana

Inaugural address by Maj. Gen. K. K.

Ohri, AVSM (Retd.), Pro-Vice

Chancellor, AUUP, Lucknow Campus

Address by Prof. Dr. Q. Rahman,

Dean Research (S & T), AUUP,

Lucknow Campus

Address by Dr. M. V. Ramana,

Director, Amity Institute of Pharmacy,

AUUP,Lucknow Campus

3. Keynote Speech 10:10-10:30 am Keynote Address by

Padmshree Dr. Nitya Anand,

Former Director, CDRI, Lucknow

4. Tea break 10.30-10:45 am Invited Lectures: Session I, Chairpersons: 1:- Dr. A. S. Negi

2:- Dr. G. Brahmachari

S. No Name of

Speaker/Designation

Time Schedule Title of Talk

IL-1 Prof. P. Pramanik 10:45-11:15 am Small and simple molecules for cancer

therapy

14. Cultural event

Management

Ms.Suchita Dubey

Ms.Dipti Srivastava

Coordination with hall management

team and preparation of events for

cultural programme.


154

IL-2 Dr. A. K. Saxena 11:15-11:45 pm Virtual screening in drug discovery

IL-3 Prof. Dr. V. K. Tandon 11:45-12.15 pm Green methodology approach to

synthesis of 1,4-napthoquinones that

potently induce apoptosis in cancer

cells.

IL-4 Prof. Rahul Jain 12.15-12.45 Synthetic histidines and their

application in the discovery of bioactive

peptides

Oral Presentations 12.45-1.30 OP1—OP4

Poster Presentations 12.30-4.30 PP1-PP50

LUNCH Session

1:30- 2:00pm

Invited Lectures: Session II, Chairpersons: 1:- Prof. P. Pramanik

2:- Prof. Dr. V. K. Tandon IL-5 Dr. Rakesh Maurya 2:00-2:30 pm Application of traditional knowledge

in search of anti-osteoporotic

potential leads from Indian medicinal

plants

IL-6 Dr. H. M. Sampath

Kumar

2:30-3:00 pm Towards the rational design of

vaccine adjuvants; dendritic cell

receptor agonists are key to new

generation designer vaccines.

IL-7 Dr. A. S. Negi 3:00-3.30 pm

Antitubulins as anticancer agents:

Inspiration from nature.

IL-8

Prof. G. Brahmachari

3.30-4.00

Practice of room temperature

synthesis: an emerging and pragmatic

chemical aspect in drug design

process

Oral Presentations 4.00-4.40 OP5-OP8

IL-9 Dr. A. K. Dwivedi 4:40-5:10 pm Spermicides as active ingredients in

barrier contraceptives

15. TEA BREAK 5:10-5:20 pm 16. CULTURAL EVENT 6:00-7:00 pm 17. DINNER 7:30 pm onwards


155

DAY-2 (25th FEB)

Invited Lectures: Session III, Chairpersons: 1:- Dr. H. M. Sampath Kumar

2:- Prof. P. Pramanik

IL-10 Dr. Ajit K. Saxena 10:00-10:30 am Isolates from Cedrus deodara

with anticancer potential

IL-11 Dr. A. K. S. Rawat 10:30- 11.00am Indian biodiversity and

bioprospecting development of

novel natural products

TEA BREAK 11:00-11:20 am

Invited Lectures: Session IV, Chairpersons: 1:- Dr. A. K. Saxena

2:- Dr. A. K. S. Rawat

IL-12 Dr. Javed Ali

11:25-11:55 am Strategy for neurological drugs:

brain delivery via intranasal

route current status and future

perspective.

IL-13

Dr. R. P. Tripathi

12:00-12:30 pm

Chemistry driven approach

towards new antitubercular

drugs

IL-14 Dr. Atul Kumar 12:30-1:00 pm Design and synthesis of new

anticancer agents

Poster Session 12.30-4.30 PP51-PP97

LUNCH 1:00- 2:00 pm

Invited Lectures: Session V, Chairpersons: 1:- Dr. Ajit K. Saxena

2:- Dr. Atul Kumar IL-15 Dr. Ram Vishwakarma 2:00-2:40 pm Chemical biology of GPI-

Anchors and new drug

discovery

IL-16 Dr. Vinod K. Tiwari 2:40-3:10 pm

IL-17 Dr. Ram Sagar Mishra 3:10-3:40 pm Efficient synthesis of

carbohydrate derived privileged

molecules


156

IL-18 Dr. Devdutt Chaturvedi 3:40-4:20 pm Greener and efficient

approaches for the syntheses of

biologically potent scaffolds.

14. VALEDICTORY /VOTE

OF THANKS

4:20-5:00 pm

15. HIGH TEA 5:00-5:30 pm

ORAL PRESENTATIONS

S.

No.

Title of Paper Name of

Presenting

Author

Oral

Poster

No.

Page

No.

1 Antimicrobial activity of

synthesized TiO2 nanoparticles

Ms. Upasna Yadav OP-1

2 In-vitro Antibacterial screening of

Andrographis Paniculata: A

possible alternative for fighting

against Mdr strains

Dr. Preeti Mathur OP-2

3 Exploration of boron tribromide as

C-C bond forming agent

Mr. Imran Ahmad OP-3

4 Total syntheses of Lawsone,

Lapachol and β-Lapachone:

Pharmacologically important

naphthoquinones

Mr. B. Satish Kumar

OP-4

5 An efficient and novel approach

for the syntheses of

dithiocarbamates from their

corresponding thiols employing

TPP.Br2

Ms. Sadaf Zaidi

OP-5

6 Synthesis, characterisation and

biological evaluation of some β-

lactam qinazolone derivatives

Ms. Deepa Lakhmani OP-6

7 Synthesis of triazine cored-sulfone

terminated dendrimers

Ms. Shazia Khanam OP-7


157

8 An efficient method for the

synthesis of substituted-1,3-

oxazolidine-2,4-diones through the

corresponding tosyloamides using

Triton-B/CO2 system

Mr. Amit K.

Chaturvedi

OP-8

POSTER PRESENTATIONS

S.

No.

Title of Paper Name of

Presenting

Author

Poster

Presentation

No.

Page

No.

1 Nephroprotective potential of

Trichosanthes Dioica R. Leaves

extract against cisplatin induced

nephropathy in Albinos

Mr. Ramesh

Kumar Gupta

PP-1

2 Multidimensional potential of

substituted benzoxazole containing

molecule in functional materials

Mr. Arun Kumar

PP-2

3 In- Silico Analysis to Access the

Antibacterial Effect Of

Schiff Bases Of Fluoroquinolones:

Molecular Docking Approach

Mr. Anup K.

Sirbaiya

PP-3

4 Green Chemistry: Solvents In The

Pharmaceutical Industry

Ms. Mehnaz

Kamal

PP-4

5 Future Prospects Of Cough

Treatment; Herbal Medicines V/S

Modern Drugs

Mr. Tarique

Mahmood

PP-5

6 Aldose Reductase Inhibitor

fidarestatas A Promising Drug Target

Inautophagy-Mediated Colorectal

Cancer: A Pilot Study

Dr. Saumya

Pandey

PP-6


158

7 Recent Advances Of Functionalized

2-Aminobenzothiazole Scaffolds

Mr. Arun Kumar PP-7

8 Antistress Potential Of Some Indian

Medicinal Plants

Ms. Aleza Rizvi PP-8

9 Quality Assurance In Herbal

Medication Mr. Doli R. Das PP-9

10 Various Polyhedral Formulations

Used For The Treatment Of Type 2

Diabetes Mellitus

Mr. Talha Jawaid PP-10

11 Efficient Synthesis Of N-Actyl

Glucosaminederived

Carbasugaranalogous For Biological

Application

Mr. Chintamv.V.S.

Narayana

PP-11

12 Ultrasonic Contrast Physics Of

Microbubbles

Dr. Kirti Bhatia PP-12

13 Synthesis And Biological Activities

Of Some Substituted Pyran

Derivatives

Dr Jaya Pandey

PP-13

14 Drug Industries And Environmental

Pollution

Dr. Richa PP-14

15 Synthesis Of Novel Substituted 4-

Thiazolidinones Derivatives

Desh Deepak

Pandey

PP-15

16 Effect of Cichorium Intybus Leaves

on N- Nitrosodiethylamine Induced

Hepatotoxicity in Wistar Rats

Ms. Neha Mathur PP-16

17 Design And Synthesis of Novel

Saponins Encompassing Tri and

Tetrasaccharide as vaccine adjuvants

Mr. Debabrata

Bhunia

PP-17

18 Development of Novel Muramyl

Dipeptide Analogues as Vaccine

Adjuvants

Mr. M. Sreekanth PP-18

19 Click Inspired Synthesis Of Diverse

Morpholine Fused 1,5-Triazoles

Mr. Soumesh

Sasi

PP-19

20 Room Temperature Synthesis Of

Phosphonate Ester Functionalized 2-

Amino-3-Cyano-4h-Chromenes Via

One-Pot Multicomponent Reaction

Dr. Goutam

Brahmachari

PP-20


159

21 Facile and Eco-Friendly Synthesis Of

3,3-Bis(Indol-3-Yl)Indolin-2-Ones

And 2,2-Bis(Indol-3-

Yl)Acenaphthylen-1(2h)-One

DerivativesAt Room Temperature Via

One-Pot Pseudo-Multicomponent

Reaction

Dr. Goutam

Brahmachari

PP-21

22 Dithiocarbamates of ω-substituted (2-

naphthyloxy) alkanes: A novel class

of antimicrobial agents

Dr. Chandan

Kumar

PP-22

23 Role of Flavonoids as Neuroprotector

in Cerebral Ischemia Mr. Abdul Basit PP-23

24 Role of Tellurium Metalloid In Drugs Dr. Sangeeta

Bajpai PP-24

25 Anti-Inflammatory And Analgesic

Activity Of Madhuca Indica Leaf

Extracts

Mr. Prakash Deep PP-25

26 A Review on Tregitopes Prediction And

Its Application As Active Pharmaceutical

Ingredients

Mr. Prateek

Shukla

PP-26

27 Deimmunization of Biotherapeutics:

Current Status And Future Prospects

Vishal Verma PP-27

28 Influence Of Standardized Aqueous

Fruit Extract Of Luffa Cylindrica On

Oxidative Stress Markers And

Limpidity Of Isolated Adult Goat

Lenses On Hydrogen Peroxide

Induced Cataract: A Possible

Alternative For Senile Cataract

Ms. Suchita

Dubey

PP-28

29 A Facile Deoxygenation Protocol of

Benzylic Alcohols Using

Bis(Benzotriazole)Methanethione As

An Vital Synthetic Auxiliary

Mr. Anoop Singh PP-29

30 Role of Computer Aided Drug

Design In Drug Development

Dr. Zeeshan

Fatima

PP-30

31 Pharmacological Screening Of Anti-

Ulcer Activity Of Saraca Indica In

Experimental Animals

Ms. Azmi Lubna PP-31

32 Hepatoprotective Property And DNA

Protection Activity Of Keramua As

Natural Product

Ms. Upma Singh

PP-32


160

33 Phytochemical Screening OfLaunaea

Procumbens For Their Biological

Activity

Ms. Preeti Rawat PP-33

34 Evaluation of The Gelling Behaviour Of

Different Natural Gums For Its

Formulation Prospects

Mr. Rachit

Mohan

PP-34

35 The Anti-Aging Molecule: Vitamin-E Ms. Parul

Tripathi

PP-35

36 Indicator Of Foreign Invasion To The

Human Body: Histamin

Mr. Vipul Verma PP-36

37 Biosensors To Be A Potential Technique

For Medical Applications Mr. Adrija

Chowdhury

PP-37

38 Biopesticides : Novel Substitutes To

Chemical Pesticides Ms. Maitreyi

Mishra

PP-38

39 Evaluation Of Anthelmintic Activity Of

Various Extracts OfAnnona Squamosa

Bark.

Mr. Sandeep

Sachan

PP-39

40 Evaluation Of Hepatoprotective

Activity of Acacia Nilotica (Bark) On

Paracetamol Induced Hepatotoxicity.

Ms. Pritt Verma PP-40

41 Performance Enhancing Traditional

Medicines In Sports

Ms. Ila Shukla PP-41

42 Production of A Novel Thermoplastic

From Pseudomonas Aeruginosamtcc

7925: A Boom For Pharmaceutical

Industry

Mr. Akhilesh

Kumar Singh

PP-42

43 An efficient and novel approach for

the syntheses of S-alkyl

thiocarbamates from their

corresponding alcohols employing

TPP.Br2

Ms. Neha Singh

PP-43

44 In-Vitro Antioxidant Activity &

Elemental Analysis

OfBauhinia.Purpureal. For Its Potential

Use In Nutraceuticals

Mr. Abhishek

Gupta

PP-44

45 Evaluation Of Jatropha Glandulifera

Extracts For Anti-Inflammatory

Activity And Wound Healing

Potential

Ms Jyotsna

Dwivedi

PP-45

46 Concomitant Administration Of

Trikatu With Curcumin As Poly

Ms. Monika

Sharma

PP-46


161

Herbal Phytoformula For Cancer

Chemotherapy

47 Characterization Of Chemical

Constitutions Of Boenninghausenia

Albiflora And Their Antioxidant

Activity

Mr. Siddharth

Pragyadeep

PP-47

48 In Vitro Antioxidant Activity On

Different Extracts Of Caesalpinia

Bonducella Seeds

Mr. Shikhar

Verma

PP-48

49 Role Of Preclinical Drug Screening To Speed Drug Discovery And

Development Processes

Mr. Pratik Khanal PP-49

50 Combinatorial Chemistry : A Tool

For Drug Discovery And Lead

Optimisation

Ms. Vandana

Singh

PP-50

51 Increasing The Efficacy Of

Diferuloylmethane As Anticancer

Agent By Increasing Solubility

Through Nanosization

Ms. Mohini

Chaurasia

PP-51

52 Formulation And Development Of In

Situ Gel For Opthalmic Drug

Delivery

Ms. Dipti

Srivastava

PP-52

53 Identification of Novel Anticancer

1,4,5-Trisubstituted 1,2,3-Triazoles

With Β-Amino Alcohol Scaffold As

Potent Antimalarial Agents.

Mr. N. Devender PP-53

54 A Strategy For The Synthesis Of

Anthraquinone-Based

Aryl‑C‑Glycosides

Mr. Kartikey

Singh

PP-54

55 In Vitro Antioxidant Activity On

Different Extracts Of Caesalpinia

Bonducella Seeds

Mr. Shikhar Verma PP-55

56 Evaluation Of In Vitro Antioxidant

Activity In Four Nephrolepis Species

Ms. Shweta

Singh

PP-56

57 Assignment And 3d Structure

Determination Of Ubiquitin From

nmr Data

Ms. Tahmeena

Khan

PP-57

58 Synthesis And Characterization of

Some Schiff Base Analogs of Novel

Piperidino Tiophenes

Dr. Sajal

Srivastava

PP-58

59 Biosensors In Cancer Diagnosis Ms. Shilpi

Srivastava

PP-59


162

60 Nanobiotechnology and Drug

Delivery: New Avenues

Ms. Shilpi

Srivastava

PP-60

61 Nanocarrier: An Effective Mean to

Integrate Phytochemical For

Enhanced Bioavailabilty And

Efficacy

Dr. Himani

Awasthi

PP-61

62 Preparation & Evaluation Of Solid

Lipid Nanoparticles Of Norfloxacin

for Ocular Delivery

Mr.Wasim Khan PP-62

63 Effect Of Catharanthus And Lemon

Grasson the Scavenging And Redox

System Of Human Blood Platelets.

Ms. Ananya

Mishra

PP-63

64 In Vitro Free Radical Scavenging

And Total Antioxidant Potential Of

Crotalaria Juncea L. Seeds

Mr. Jamal A.

Ansari

PP-64

65 Evaluation Of In Vitro Antioxidant

Activity Of Anthocephalus Cadamba

(Roxb.) Miq Bark Fractions

Ms. Nishat

Fatima

PP-65

66 Evaluation Of Antioxidant Potential

Of Swertia Chirayata L

Ms. Homa Jilani

Khan

PP-66

67 Therapeutic Potential Of

Thymoquinone :An

Active Phytochemical Of Nigella

Sativa

Md S. Iqbal

PP-67

68 Folate- a double-edged sword in

cancer

Ms. Apeksha

Srivastava

PP-68

69 Review on Techniques For

Enhancement of Solubility of Statins

Ms. Richa

Srivastava

PP-69

70 Folate Targeted (Nano) Drug

Delivery Systems Using Folate as a

Targeting Ligand

Ms. Richa

Srivastava

PP-70

71 Development of Nano-Self

Emulsifying DrugDelivery System for

Antimalarial Treatment

Ms. Richa

Srivastava

PP-71

72 Organogels: Trending Novel Drug

Delivery System

Mr. Rahul

Kushwaha

PP-72

http://en.wikipedia.org/wiki/Phytochemical

http://en.wikipedia.org/wiki/Nigella_sativa



163

73 Liposomes:An Advacement in Novel

Drug Delivery systems

Ms. Nishita Singh PP-73

74 Role of Community Pharmacist in

Healthcare of the Society

Mr. Abhishek

Nayak

PP-74

75 An efficient, one-pot, syntheses of

trithiocarbonates through

corresponding alkyl halides

employing Cs2CO3/CS2 System

Mr. Nitin

Srivastava

PP-75

76 Dithiocarbamates of ω-substituted (2-

naphthyloxy) alkanes: A novel class

of potential antioxidant agents

Ms. Sadaf Zaidi PP-76

77 An efficient method for the synthesis

of substituted-1,3-oxazolidine-2,4-

diones through the corresponding

haloamides using Triton-B/CO2

system

Dr. Amit K.

Chaturvedi

PP-77

78

An efficient method for the syntheses

of β-substituted alkyl carbamates

through the Michael addition

approach

Ms. Sadaf Zaidi

PP-78

79 Insecticidal activity of

dithiocarbamates of ω-substituted (2-

naphthyloxy) alkanes

Ms. Sadaf Zaidi PP-79

80 Molecular interaction of Survivin and

naturally occurring ligands by Insilico

analyses for retinoblastoma targeting

Mr. Ajita Trivedi PP-80

81 Synthesis and anti-inflammatory

activity of pyrazole based compound

Ms. Praveen

Singh

PP-81

82 Design and Synthesis of 2-Pyridone

Based Flexible Dimers and Their

Conformational Study through XRD

and DFT: Perspective of

Cyclooxygenase-2 Inhibition

Mr. Sunil K. Rai PP-82

83 Synthesis and Self Assembly of

Tripodal Supramolecular Architecture

Ms. Archana

Gaurav

PP-83


164

84 Synthesis and antimicrobial

evaluations of diarylchromene

analogs

Mr. Parmesh K.

Dwivedi

PP-84

85 Dithiocarbamate derivatives of

zerumbone: A novel class of

antimicrobial and anticancer agents

Mr. Parmesh K.

Dwivedi

PP-85

86 Entinostat a ray of hope in breast cancer Mr. Pragyandip

P. Dash

PP-86

87 Evaluation of anti-inflammatory

activity of methanolic extract of

Haldina cordifolia

Mr. Pragyandip

P. Dash

PP-87

88 Synthesis of Primaquine Glyco-

conjugates at physiological pH as

potential tissue-schizontocidal

antimalarial agents

Dr. Saxena M.

PP-88

89 A new triterpene from the leaves of

Ceriops Tagel

Dr. Rajesh

Kumar

PP-89

90 Formulation & Evaluation of

Chronomodulated drug delivery

system of an Anti –inflammatory

drug

Ms. Sarita Pal PP-90

91 Pharmacological and Bio-Molecular

Investigation of Curcumin for Anti-

asthmatic Activity

Mr. Saikat Sarkar PP-91

92 Design of Some Novel Aromatic

Amides AgainstAdes Aegpti

Mosquitoes

Dr. Akansha

Garud

PP-92

93 Treatment of Lifestyle Disorders by

Herbal Medication

Ms. Richa

Srivastava

PP-93

94 Synthesis of Benzenepropanamine

Analogs as possible spermicides

Ms Anjali Mishra PP-94

95 Synthesis of 1-dialkylamino

carbodithioc Acid S-[(2,3

Epithio)Propyl] ester and derivatives

having spermicidal activity

Mr. Suyash

Tiwari

PP-95


165

96 Treatment of Lifestyle Disorders by

Herbal Medications

Ms. Richa

Srivastava

PP-96

97 Stereoselective total synthesis of

cytotoxic oxylipin Topsentolide B2

Dr. Devdutt

Chaturvedi

PP-97

98 Characterization of macrocyclic

complexes synthesized by

sonochemical method: A green

approach

Dr. Monika

Kamboj

PP-98

INVITED

LECTURES IL-1

Small and simple molecules for cancer therapy

P. Pramanik (Ex-professor of IIT, Kharagpur)

Department Basic Science, MCKV Institute of Technology, Liluah, Howrah 711204, W.B.

Cancer is becoming an epidemic all over the world. It is more serious problem for developing

countries like India because major patients are below poverty line. It is a serious need for scientific

world to invent some simple cheap drug. In this regard, most outstanding contribution came from

the drug used by Nobel Laureate William Koch who used some mixture of glyoxal and

methyl-glyoxal with reasonable success . He practiced this medicine in the name of homeopathy.

After his departure from medical field due to some social injustice , Nobel Laureate Albert

Szent-Gorgydiscovered that methyl glyoxal is present in blood and is responsible to protect us

from cancer disease ..It is also very interesting to note that many copper compounds have

excellent anticancer activities which may be comparable with compounds of Platinum and

other higher transitional elements . It should not be ignored that Nobel Lauriate Linus Pauling

advocated the high doses of Vitamin C for prevention of cancer usurping the works of two


166

scientists, Albert Szent-Gorgy and Irwin Stone This paper will present the possible simple

therapies and preventives from simple molecules for battle with cancer disease .

IL-2

Virtual Screening in Drug Discovery

Anil K. Saxena.

Division of Medicinal and Process Chemistry, CSIR-Central Drug Research Institute, Lucknow, India-

226001

Email:[email protected]

The identification and optimization of molecules as new drug candidates through biological target

identification and validation using multidisciplinary approaches are of key importance in the drug

discovery process. The traditional approaches to drug discovery had also been based on the leads

either from natural products or from the fragments/substructures from the known active molecules

through pattern recognition. The recent advancements in the area of genomics, proteomics and

computational technology drug discovery process have gained dramatic momentum as

understanding and dissection of multi factorial diseases can be performed at molecular level. The

collective approach using genomics, proteomics and computational techniques has a great

potential in accelerating the process of drug discovery. The dramatic complexity in the process of

drug discovery and development has enlisted it as one of the expensive, challenging and time

consuming task. The process of rational drug design involves the CADD (Computer Aided Drug

Design) techniques both for direct (target structure is known) and indirect (target structure is

unknown) design. The mathematical models derived through QSARs (Quantitative Structure –

Activity Relationships), pharmacophors and docking studies using CAMM (Computer Aided

Molecular Modeling Techniques) are predictive. In virtual screening theses models are used for

finding new hits and prioritizing the molecules for their synthesis. Virtual screenings has great

potential in the repositioning of the existing generic drugs. The application of virtual screening for

focused libraries in case of anti Alzheimer agents1-3 has been rewarding in the invention of

potential molecules more effective than the existing ones.

References:

1. Chaudhaery SS, Roy KK, Shakya N, Saxena G, Sammi SR, Nazir A, Nath C, Saxena A

K,J. Med. Chem. 2010, 53, 6490.


http://www.ncbi.nlm.nih.gov/pubmed/?term=Chaudhaery%20SS%5BAuthor%5D&cauthor=true&cauthor_uid=20684567

http://www.ncbi.nlm.nih.gov/pubmed/?term=Roy%20KK%5BAuthor%5D&cauthor=true&cauthor_uid=20684567

http://www.ncbi.nlm.nih.gov/pubmed/?term=Shakya%20N%5BAuthor%5D&cauthor=true&cauthor_uid=20684567

http://www.ncbi.nlm.nih.gov/pubmed/?term=Saxena%20G%5BAuthor%5D&cauthor=true&cauthor_uid=20684567

http://www.ncbi.nlm.nih.gov/pubmed/?term=Sammi%20SR%5BAuthor%5D&cauthor=true&cauthor_uid=20684567

http://www.ncbi.nlm.nih.gov/pubmed/?term=Nazir%20A%5BAuthor%5D&cauthor=true&cauthor_uid=20684567

http://www.ncbi.nlm.nih.gov/pubmed/?term=Nath%20C%5BAuthor%5D&cauthor=true&cauthor_uid=20684567

http://www.ncbi.nlm.nih.gov/pubmed/?term=Saxena%20AK%5BAuthor%5D&cauthor=true&cauthor_uid=20684567



167

2. Roy KK, Tota S, Tripathi T, Chander S, Nath C, Saxena AK. Bioorg Med Chem, 2012, 20

, 6313

3. Chaudhaery SS, Roy KK, Saxena AK, J. Chem. Inf. Model., 2009, 49 , 1590.

IL-3

Green methodology approach to synthesis of 1,4- naphthoquinones that

potently induce apoptosis in cancer cells.

Vishnu K. Tandon

Department of Applied Sciences, Institute of Engineering and Technology, U.P. Technical University,

Lucknow-226020, U. P.

Green chemistry has been recently receiving considerable attention by major scientific discipline1

and water is universal solvent for various syntheses with respect to green chemistry principles2. This

has motivated us to develop a green methodology to synthesize 1,4- naphthoquinone derivatives

which potently induce apoptosis in human cancer cells3. The synthetic route and anticancer activity

of these compounds will be discussed in detail.

References:

1. Dallinger, D.; Kappe, C. O. Chem.Rev. 2007, 107, 2563.

2. Herrerias, C.I.; Yao, X.; Li, C.-J. Chem.Rev.2007, 107, 2546.

3. Tandon, V.K.; Kumar, S. Expert Opin. Ther. Patents, 2013, 23, 1087. (U.K.).

IL-4

Synthetic histidines and their application in the discovery of bioactive peptides

Rahul Jain

Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research,

Sector 67, S. A. S. Nagar, Punjab 160 062, India



http://www.ncbi.nlm.nih.gov/pubmed/?term=Tota%20S%5BAuthor%5D&cauthor=true&cauthor_uid=23026084

http://www.ncbi.nlm.nih.gov/pubmed/?term=Tripathi%20T%5BAuthor%5D&cauthor=true&cauthor_uid=23026084

http://www.ncbi.nlm.nih.gov/pubmed/?term=Chander%20S%5BAuthor%5D&cauthor=true&cauthor_uid=23026084

http://www.ncbi.nlm.nih.gov/pubmed/?term=Nath%20C%5BAuthor%5D&cauthor=true&cauthor_uid=23026084


http://www.ncbi.nlm.nih.gov/pubmed/?term=Chaudhaery%20SS%5BAuthor%5D&cauthor=true&cauthor_uid=19441865




168

With the increasing importance of enzymes and peptide hormones as targets for biological

intervention, the synthetic derivatization of the genetically coded amino acids and their

incorporation into peptides has become one of the attractive strategies for the preparation of

hormone agonist/antagonists and enzyme inhibitors of pharmacological importance. Five

membered rings containing more than one heteroatom constitute one of the largest and most

diverse groups of heterocyclic compounds. Among this class, the imidazole ring system has special

biological importance, in large part because of its presence in the essential amino acid histidine

and in histamine, the decarboxylated product of histidine. The physicochemical properties of the

side-chain imidazole ring, its acid-base characteristics, aromaticity, hydrogen bond donor/acceptor

properties and ring tautomerism makes histidine a unique DNA encoded α-amino acid.

This presentation shall provide an overview of the chemistry of synthetic histidines, and their

application in the synthesis of potent bioactive peptides.

Selected References:

1. Mahindra, A.; Bagra, N.; Wangoo, N.; Khan, S. I.; Jacob, M. R.; Jain, R. Discovery of short

peptides exhibiting high potency against Cryptococcus neoformans. ACS Med. Chem. Lett. 2014,

5, 315-320.

2. Mahindra, R.; Jain, R. Regiocontrolled palladium-catalyzed and copper-mediated C-H bond

functionalization of protected L-histidine. Org. Biomol. Chem.2014, 12, 3792-3796.

3. Mahindra, A.; Bagra, N.; Jain, R. Palladium-catalyzed regiospecific C-5 arylation of protected

L-histidine: Microwave-assisted C-H activation adjacent to donor arm. J. Org. Chem., 2013, 78,

10954-10959.

4. Sharma, R. K.; Reddy, R. P.; Tegge, W.; Jain, R. Discovery of Trp-His and His-Arg analogues

as new structural classes of short antimicrobial peptides. J. Med. Chem., 2009, 52, 7421-7431.

5. Engel, S.; Neumann, S.; Kaur, N.; Monga, V.; Jain, R.; Northup, J.; Gershengorn, M. C. Low

affinity analogs of thyrotropin-releasing hormone are super-agonists. J. Biol. Chem. 2006,

281,13103-13109.

6. Kaur, N.; Lu,X.; Gershengorn,M. C.; Jain, R. Thyrotropin-releasing hormone (TRH) analogues

that exhibit selectivity to TRH receptor subtype 2. J. Med. Chem., 2005, 48, 6162-6165.

IL-5

Application of Traditional Knowledge in Search of Potential Leads for the

Treatment of Osteoporosis

Rakesh Maurya

Medicinal and Process Chemistry Division


169

Central Drug Research Institute, CSIR, Lucknow 226 001, India


Osteoporosis is now widely recognized as a public health problem. This disease which increases

bone fragility and thereby the risk of fractures, is associated with high mortality, morbidity and

medical expenses throughout the world. Considering the broad spectrum effect of osteoporosis in

the medical system, currently an increasing demand is sought in the alternative system of medicine

to design strategies to prevent and cure this devastating ailment. There is a large variety of plants

in the traditional system of medicine for the treatment of bone disorders. But the systematic

identification of lead molecules has not been made. We have identified osteogenic lead molecules

from traditional plant. These leads when administered to ovariectomized rats significantly

increased the bone mineral density. Some aspects of our recent research with natural products of

plant origin directed to the treatment or prevention of osteoporosis will be presented.

IL-6

Towards the rational design of Vaccine Adjuvants; dendritic cell receptor

agonists are key to New Generation Designer Vaccines

Halmuthur M. SampathKumar

Indian Institute of Chemical Technology (CSIR-IICT), Hyderabad-500007, India

E mail: [email protected]

Finding safe efficacious adjuvants in order to enhance immune responses against target

immunogens has been a major and recurrent issue for the vaccine industry. This is still an unsolved

challenge, most particularly in the context of a growing interest in designing new types of vaccines

capable of eliciting Th1 immune responses. Importantly, recent advances in our understanding of

the physiology of immune responses offer new avenues to design and test candidate adjuvants,

based on either synthetic or natural molecules, with the aim to mimic and recapitulate pro-

inflammatory signals initiating both innate and adaptative immune effector mechanisms. Of the

novel compounds recently evaluated in human trials, immunostimulatory molecules such as the

lipopolysaccharide derived MPL and the saponin derivative QS21 appear most promising,

although doubts have been raised as to their safety in humans. Thus, adjuvants of the future might

be highly designer synthetic molecule encompassing immune stimulatory molecular patterns of

pathogens together with the structural elements that act as delivery vehicles for vaccines which

attract, target or activate professional antigen presenting cells. When used alone or in combination,

such molecules should facilitate antigen presentation by professional APCs and lead to a potent


170

induction of T cell-mediated effectors and immune memory mechanisms. An overview of the new

generation vaccine adjuvants based on pathogen associated molecular patterns, their mechanism

of action and merits shall be presented.

IL-7

Antitubulins as anticancer agents: Inspiration from nature

Arvind Singh Negi

CSIR-Central Institute of Medicinal and Aromatic Plants, P.O. CIMAP, Kukrail Picnic Spot Road,

Lucknow-226015, India.


Keywords: antitubulins, microtubule stabilizers, microtubule destabilizers, anticancer

ABSTRACT

Cancer is a public menace. According to WHO, cancer alone caused 13% of total human

deaths in 2012 [1]. The morbidity and mortality of cancer is so high that it has become a challenge

to our healthcare system. The complexity of the disease is too much and still today, cancer is a

challenge. Nevertheless, researchers are exploring all possibilities to tackle the problem.

Microtubules, a globular protein are a rigid hollow cylinders built by polymerization of tubulin

dimmers. Microtubules are considered as an attractive target in cancer chemotherapeutics. Tubulin

‘polymerisation-depolymerisation’ is an essential process which is known as ‘microtubule

dynamic instability’. Microtubules play a key role in various cellular processes including mitosis.

Any interference in microtubule dynamics has a significant impact on cell division which

ultimately causes cell death. Compounds either stabilizing or inhibiting microtubule assembly,

interfere in microtubule dynamics are known as antitubulins [2]. In both the cases the equilibrium

of this process is disturbed which ultimately induces cell death. Paclitaexl, epothilones,

laulimalide, peruloside and descodermolide are microtubule stabilizers while podophyllotoxin,

combretastatins, vinca alkaloids, dolastatins etc. are microtubule destabilizers. We have designed

and synthesized several pharmacophores as antitubulins based on structure activity relationship of

some natural antitubulins. Their basis of designing, chemical syntheses and biological evaluation

will be discussed in detail [3].



171

O

HN

H3CO

H3CO

H3CO

C CH3

OA B

C

Colchicine

OCH3

OCH3

H3CO

H3CO

OCH3

OH

Combretastatin A4

O

OCH3

OCH3

H3CO

O

O

O

OH

Podophyllotoxin

OCH3

H3CO

H3CO

Antitubulin effect

3,4,5-Trimethoxyphenyl unit

References

[1] WHO, Cancer factsheet No 297, February 2014.

[2] Negi, A. S. et al. Bioorg. Med. Chem. 2015, 23: 373-389.

[3] Parihar, S. et al. J. Steroid Biochem. Molecular Biol. 2013,137: 332– 344.

IL-8

Practice of Room Temperature Synthesis: An Emerging and Pragmatic

Chemical Aspect in Drug Design Process

Goutam Brahmachari

Laboratory of Natural Products and Organic Synthesis, Department of Chemistry, Visva-Bharati (a

Central University), Santiniketan-731235, West Bengal, India

E-mail: [email protected]; [email protected]

It is needles to mention that a successful tie-up between chemistry and biology is the basis of drug

design and discovery! Drug discovery process is a continuing endeavor by the scientists working

in these multi-disciplinary areas of tremendous scientific attention to save and improve of the

quality of human life. ‘Interfacing Chemical Biology & Drug Design (ICBDD-2015)’ is thus a

timely-organized scientific platform where scientists from various disciplines can meet together,

interact and exchange their views that would surely boost the ongoing research in this direction.

As mentioned above, drug discovery programme is a multi-step process involving

numerous groups of individuals working in disciplines ranging from the basic sciences to the

medical and legal professionals. In practice, a drug is most likely an organic small molecule that

activates or inhibits the function of a biomolecule (e.g. DNA, RNA, protein, and enzyme), which

in turn results in a therapeutic benefit to the patient. A drug target is the key molecule involved in

a particular metabolic or signaling pathway that is specific to a disease condition or pathology or

to the infectivity or survival of a microbial pathogen. Drug design or ligand design usually involves

the design of small molecules that are complementary in shape and charge to the biomolecular

target with which they interact and therefore will bind to it. Among such small molecules, natural

products or products obtained from them through synthesis have been successfully playing the



172

leading role in the history of medicine! Synthesis of natural products-inspired and biologically

relevant small molecules has also found to be effective in this domain during the last several

decades.

Synthetic organic chemists from the basic field of research have also been playing a crucial

role in the entire process through supplying a plenty of organic small molecules having a wide

range of structural variations in a regular fashion in the purpose of pharmacophore identification

and/or modification as an initial step of drug discovery process. In this context, practice of Green

Chemistry has already emerged as a distinct field of research. Amongst the so-called ‘The Twelve

Principles of Green Chemistry’, ‘design for energy efficiency’ is noteworthy! The essence of this

principle is ‘energy requirements should be recognized for their environmental and economic

impacts and should be minimized. Synthetic methods should be conducted at ambient temperature

and pressure’ and thus facilitates to maintain the sustainability of our beloved planet! During large-

scale industrial production, energy usage is really a vital concern. In addition, room temperature

condition is the mildest reaction condition, essentially required for many temperature-sensitive

organic substrates as a key step in multi-step sequence reactions. That is why, as a part of on-going

developments on green synthetic strategies, designing for room temperature conditions coupled

with other green aspects is also an area of current choice. Energy, like thinking about how to

arrange a synthesis to have the fewest number of steps, or use the lowest cost starting materials or

any other aspect of interest to the synthetic or process chemist, is just another design parameter.

Now time has come we can no longer afford to design new molecules in the absence of a detailed

and extended consideration of how energy will be used! The talk will focus on such emerging field

highlighting some of the recent works from the Laboratory of the present investigator in this

direction.

IL-9

Spermicides as active ingredients in barrier contraceptives

Dr. Anil Kumar Dwivedi

Division of Pharmaceutics, CSIR-CDRI, Lucknow, INDIA

According to an estimate, ~40% of all pregnancies that occurred worldwide were unintended,

which strongly indicates that the available methods of contraception are insufficient to cater the

unmet need of millions of couples. Barrier contraceptives containing spermicides have the

potential to be a valuable addition to the “menu” of choices available to women to take control of

their reproductive activity.Nonoxynol-9 (N-9), a detergent with potent spermicidal properties is

used as an active ingredient in many spermicidal preparations. However, multiple use of N-9

spermicide may cause irritation to the vagina and rectum, increasing the chance of HIV and STD

infections in users. Our Institute has developed and licensed a vaginal contraceptive cream


173

(CONSAP) which contains saponins isolated from the fruit pericarp of the plant Sapindus

mukorossi as the active ingredient.

Several thymol derivatives, systems having αβ-unsaturated ketonic groups, curcumin

derivatives, substituted butyrolactones were preparedand evaluated for their spermicidal activity.

Details will be discussed in the conference.

IL-10

Isolates from Cedrus deodara with anticancer potential

A. K. Saxena

Amity University Uttar Pradesh, Lucknow - 226028

Cedrus deodara (Himalayan cedar, ‘devadaru’; family: Pinaceae) is a highly reputed Indian

Medicinal plant. The plants have been used as a source of medicine since times immemorial and

many of the anticancer drugs in clinical use for the treatment of cancer have derived from plants.

A standardized fraction has been derived from heart wood of C. deodara comprising of (-)-

Matairesinol (9 to 13%), (-)-Wikstromol (75 to 79%) Dibenzylbutyrolactol (7 to 11%) and

unidentified material (2.6 to 3%).

In vitro cytotoxicity studies using standardized fraction (10, 30 and 100 microgram / ml) showed

significant dose dependent effect against several human cancer cell lines from different tissues.

The IC50 values (microgram / ml) observed for different cell lines were breast: MCF-7 (15.6), T-

47 D (9.78); CNS: SF-539 (29.09), SKNMC (0.0164), IMR-32 (52.74), SKNSH (41.67), SNB-78

(28.35); cervix: Hela (39.0), SiHa (8.3); colon: Colo-205 (5.4), HCT-15 (21.05), HT-29 (12.24),

SW-620 (40.9) and liver: HEP-G2 (116.03). Comparative data of in vitro cytotoxicity against

human cancer cell lines also showed synergistic effect of the standardized fraction in comparison

to individual molecules present in standardized fraction.

The in vivo anticancer activity in murine models was determined and animals were treated with

standardized fraction for nine days (i.p.). The results showed 53% and 54% tumor growth

inhibition in Ehrlich tumor (solid) at 250 and 300 mg/kg (i.p.) respectively. The tumor growth

inhibition in CA-51 Colon carcinoma at 400 mg/kg (i.p.) was 54%. When the animals were treated

with lowed dose of standardized fraction (150 mg/kg, i.p.) alongwith piperine (20 mg/kg, i.p),

46.43% tumor growth inhibition was observed in Ehrlich tumor (solid) model. The piperine

showed beneficial effect on tumor growth inhibiting properties of standardized fraction.

Standardized fraction (10, 30 and 100 microgram / ml) increased the percentage of annexin

V positive HL-60 cells to 1.9 - 17.18% as compared to control (1.04%). Standardized fraction (10,

30 and 100 microgram / ml) and staurosporine (1 micromolar) showed 9.13%, 11.38%, 17.22 %

and 28.07% intacellular caspases activation respectively in K562 cells . Standardized fraction also


174

produced distinct DNA ladder pattern in HL-60 and K562 (30 and 100 microgram / ml) and

MOLT-4 cells (30 microgram / ml) after 24 hrs incubation. DNA cell cycle analysis indicated that

Standardized fraction (10, 30 and 100 microgram / ml) increased the content of hypodiploid (sub

G1 phase) cells when compared to control (2.55, 5.4 % and 6.25 % vs. 0.27 % respectively).

The present study indicates that Standardized fraction derived from heart wood of Cedrus

deodara has cytotoxic potential against human cancer cell lines. It has capability to induce tumor

growth inhibition in vivo and induces apoptosis as indicated by annexin V positive cells, induction

of intracellular caspases, DNA fragmentation and DNA cell cycle analysis.

IL-11

INDIAN BIODIVERSITY AND BIOPROSPECTING FOR DEVELOPMENT OF NOVEL

NATURAL PRODUCTS

A.K.S. Rawat

Pharmacognosy & Ethnopharmacology Division

CSIR-National Botanical Research Institute, Rana Pratap Marg, Lucknow (India)

Ph.: +91 522 2297816, Fax: +91 522 225836; Email: [email protected]

India is one among the top 12 mega biodiversity countries in the world. The rich biodiversity and

the associated traditional knowledge systems are the two major components, which India can

utilize profitable to generate a number of natural products and technologies. Biodiversity as a

source of new knowledge, innovations and ideas, capable of generating IPR protected technologies

in the area of herbal drug development is increasing. In this changing world scenario, it is important

to analyze the strengths and weaknesses of India in respect of new IPR regime. There has been an

increasing realization that the green medicine is safer and this has led to the spurt in the use of

plant based medicines across the world and in India too. The global herbal market is about US$

90 billion which is growing at the rate of 10-15% annually and is expected to cross 5 trillion US$

by 2030. The traditional medicine in India functions through two streams i.e. the folk stream and

the classical organized stream that includes the Ayurveda, Unani, Siddha etc. The folklore

medicine is again routed either through the rural village based or the tribal based. Thus the use of

medicinal plants amounts to around 8000 wild plants in these medicines. Although the global

market of herbal drug is growing at a fast pace, the Indian share is only 2%. The major reason for

this being the lack of proper quality, safety and efficacy of herbal drugs despite having in-depth

knowledge in ayurvedic medicinal system. There are opportunities in 21st century for developing

countries like India with traditional knowledge base to develop globally acceptable newer

Ayurvedic drugs/neutraceuticals and convert their rich bio-resources & associated traditional

knowledge systems & for economic wealth & thereby bring prosperity to the nation.


175

Indian herbal drug industries generally face the problem of adulteration & substitution. The

lack of confidence in the quality of drug in traditional medicine in hindering us from capitalizing

these systems at global level. It is well documented that the quantity and nature of secondary

metabolites in medicinal plants is influenced by growth, season, edaphic and environmental

factors.Therefore, there is a need to develop quality parameters of raw drugs, proper collection and

processing along with HPTLC/HPLC finger printing to get desirable quality of raw material.

In the whole process development of herbal drug/product based on traditional knowledge needs

proper taxonomically identified safe raw material and scientific validation of the products. Further

get constant supply of right raw material whether procured from wild or cultivated and their storage

one has to follow. Good Agriculture Practices (GAP), Good Collection Practices (GCP), Good

Ethical Practices (GEP), Good Procurement Practices (GPP), Good Safety Practices (GSP)

[Pesticide, heavy metal, microbial load as per WHO guidelines] and Good Storage Practices

(GSP).

IL-12

“Strategy for neurological drugs: brain delivery via intranasal route current

status and future perspective”

Javed Ali

Department of Pharmaceutics, Faculty of Pharmacy, Jamia Hamdard, Hamdard Nagar, New Delhi

E. mail address: [email protected], [email protected]

The blood brain barrier (BBB) represents an insurmountable barrier for the majority of drugs.

Diseases of the Central Nervous System (CNS) are particularly challenging because of delivery of

therapeutics across the BBB. Consequently, due to its restricted permeability it prevents the use of

many therapeutic agents because of the inability of the agents to reach and maintain effective

concentration in the brain for an appropriate length of time. The transport of exogenous materials

directly from nose-to-brain is a potential route for by-passing the BBB. This route, involves the

olfactory or trigeminal nerve systems which initiate in the brain and terminate in the nasal cavity

at the olfactory neuroepithelium or respiratory epithelium. They are the only externally exposed

portions of the CNS and therefore represent the most direct method of non-invasive entry into the

brain. The potential for both interesting treatment possibilities and the risk of unwanted side effects

associated with olfactory transfer of drugs will increase as more effective formulations and

delivery devices are developed. Recently the apomorphine hydrochloride dry powders have been

developed for intranasal delivery (Apomorphine nasal, Lyonase technology, Britannia

Pharmaceuticals, Surrey and U.K). The results of clinical trial Phase III suggested that the prepared

formulation had clinical effect equivalent to subcutaneously administered apomorphine. The

conventional way of administering the drugs to intranasal route includes solutions, sprays, and


176

suspensions however because of its obvious disadvantages, the incorporation of drugs into

nanoparticulate formulations are being investigated extensively. Since colloidal formulations have

been shown to protect them from the degrading milieu in the nasal cavity and facilitate their

transport across the mucosal barriers. The brain gets benefited through the intranasal delivery as

direct olfactory transport bypasses the blood brain barrier and nanoparticles are taken up and

conveyed along cell processes of olfactory neurons through the cribriform plate to synaptic

junctions with neurons of the olfactory bulb. The intranasal delivery is aimed at optimizing drug

bioavailability for systemic drugs, as absorption decreases with increasing molecular weight, and

for drugs, which are susceptible to enzymatic degradation such as proteins and polypeptides. The

research findings from the research lab with respect to development of polymeric nanoparticles,

solid lipid nanoparticles, nanoemulsions and nanolipid carriers would be discussed for efficient

delivery of actives to brain and hence achieving high benefit to low risk ratio as compared to

conventional delivery. Although many, challenges remains ahead, the increasing knowledge about

the nanoparticulate drug delivery via nasal administration is a growing field.

Suggested References:

1. Shadab Md, Shadabul Haque, Mohd Fazil, Manish Kumar, Sanjula Baboota, Jasjeet K Sahni,

Javed Ali, “Optimized nano-formulation of bromocriptine for direct nose to brain delivery:

Biodistribution, pharmacokinetic and dopamine estimation by UHPLC/MS method", Expert

Opinion on Drug Delivery, 11 (6) 827–842 (2014).

2. Bhavna, Shadab Md, Mushir Ali, Rashid Ali, Aseem Bhatnagar, Sanjula Baboota, Javed Ali,

“Donepezil nanosuspension intended for nose to brain targeting: In vitro and In vivo Safety

Evaluation”, Int. J. Bio. Macromolecules 67, 418–425 (2014).

IL-13

Chemistry Driven Approach towards New Antitubercular Drugs

R. P. Tripathi

Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute

Lucknow-226001, India

Email: [email protected], [email protected]

Tuberculosis caused by mainly by M. tuberculosis in humans claims millions of lives each year

globally. The arsenal of current existing drugs is becoming redundant due to emergence of MDR

and XDR strains. Moreover, only limited number of molecules exists today in drug development

pipeline and they are associated with one or more drawbacks. To overcome the problems

associated with tuberculosis control remedies there is an urgent need of new drugs or drug


177

combination to treat tuberculosis effectively in cost effective manner. Traditional drug

development guided by chemistry of late has been overtaken by biology and different mechanical

tools. This approach as well as the strict regulations has resulted in reduction of new chemical

entities. The future of drug discovery process is thought to lead an enhancement in new chemical

entities only by chemistry driven strategies. Our group at CSIR-CDRI has taken an initiative to

develop new antitubercular agents involving simple, economical and echo-friendly synthesis of

phenyl cyclopropyl methanes and other simple compounds with potent activity. The details of

synthetic strategy and biological activities will be discussed.

References: N. Anand, K. K. G. Ramakrishna, M. P. Gupt, V. Chaturvedi, S.Singh, K. K.

Srivastava,P. Sharma, N. Rai,R.Ramachandran,,A. K. Dwivedi, V. Gupta,B. Kumar, S. Pandey,P.

K. Shukla, S. K. Pandey, J. Lal,and R.P. Tripathi ACS Med Chem Lett2013, 4(10), 958-963.V.

Kukshal, M. Mishra, A Ajay, T. Khanam, R. Sharma, D. Dube, D. Chopra, R. Ramchandran, R.P

Tripathi 2012,MedChemComm., DOI:10.1039/C2MD00168C, R. P. Tripathi, S.S. Bisht, A. Ajay,

A. Sharma, M. Misra, M. P. Gupt, Curr. Med. Chem, 2012, 19, 488-517., N. Singh, S. K. Pandey,

N. Anand, R. Dwiwedi, S. Singh, S. K. Sinha, V. Chaturvedi, N. Jaiswal, A. K. Srivastava, P.

Shah, M. I. Siddiqui, R. P. Tripathi Bioorg. Med. Chem. 2011, 21, 4404-4408, R. P. Tripathi , J.

Pandey, V. Kukshal, A. Ajay, M. Mishra, D. Dube, D. Chopra, R. Dwivedi V. Chaturvedi and R.

Ramachandran MedChemComm2011, 2, 378-384. A. Ajay, V. Singh, S. Singh, S. Pandey, S.

Gunjan, D. Dube, S. K. Sinha, B. N. Singh, V. Chaturvedi, R. Tripathi, R. Ramchandran, R. P.

Tripathi, Bioorg. Med. Chem. 2010,18, 8289-8301 S.S. Bisht, N. Dwivedi, V. Chaturvedi, N.

Anand, M. Misra, R. Sharma, B. Kumar, R. Dwivedi, S. Singh, S. K. Sinha, V. Gupta, P.R. Mishra,

A. K. Dwivedi and R. P. Tripathi Eur. J. Med. Chem. 2010, 45, 1965-1978

IL-14

Design and synthesis of new Anticancer Agents

Atul Kumar*, S. Sanyal, D. Dattac and N. Chattopadhyay

Medicinal Chemistry Division, Central Drug Research Institute, Lucknow

Employing a rational design of Thioaryl naphthylmethanone oxime ether analogs containing

functional properties of various anti-cancer drugs, a series of compounds were identified that

displayed potent cytotoxicity towards various cancer cells, out of which CDRI-MANS) exhibited

best safety profile. MANS induced apoptosis, inhibited migration and invasion, strongly inhibited

cancer stem cell population on a par with salinomycin, and demonstrated orally potent tumor

regression in mouse MCF-7 xenografts.


178

IL-15

Chemical Biology of GPI-Anchors and New Drug Discovery

Dr. Ram. A. Vishwakarma

Director, CSIR-IIIM, Jammu

(Not Attended)


179

IL-16

Synthesis of Diverse Benzothiazoles/benzoxazole and Amides via Cleavage of

Benzotriazole ring

Vinod K Tiwari

Department of Chemistry, Faculty of Science, Banaras Hindu University, Varanasi-221005

Email: [email protected]

ABSTRACT

Benzotriazole methodology, a versatile, useful, and one of the most successful synthetic protocol

investigated so far, has now grown from an obscure level to very high popularity since it can easily

be introduced into a molecule, activates it towards various transformations, remains sufficiently

stable during the reaction course, and finally can easily be removed at the end of reaction sequence.

The operational simplicity, benign biological and physical properties, ready availability, and

remarkable catalytic action in various reactions. Very recently, we have developed a concise and

efficacious benzotriazole-mediated novel two-step protocol for an easy access to glycoconjugate

benzothiazoles from protected carbohydrates. The benzotriazolemethanethione, prepared by the

reaction of free alcohol with bis(1H-benzo[1,2,3]triazol-1-yl)methanethione, on treatment with

silanes or stannane under heating or microwave irradiation undergoes free radical β-scission of N–

N bond and affords diverse range of 2-O-substituted benzothiazoles via cyclative elimination of

molecular Nitrogen. The method was extended for the synthesis of numerous 2-N/S/C-substituted

benzothiazoles from substituted thiocarbonylbenzotriazoles via free-radical intramolecular

cyclative cleavage of the benzotriazole ring in the presence of (TMS)3SiH and AIBN under mild

conditions. The developed methodology demonstrates significant compatibility under microwave

conditions and is important as it avoids the use of toxic metals for radical cyclization. Furthermore,

the chemistry has been successfully investigated for the deoxygenation and also for the

development of benzoxazoles as well amides of great chemotherapeutic values from acyl

benzotriazole under mild condition via cleavage of benzotriazole ring. Chemistry will be presented

in great detail.

References

1. (a) RR Kale, V Prasad, MA Hussain, V K Tiwari, Tetrahedron Lett., 2010, 51, 5740; (b) RR

Kale, V Prasad, V K Tiwari, Synlett, 2011, 2, 195; (c) RR Kale, V Prasad, PP Mohapatra, V K

Tiwari, Monatsh Chemie, 2010, 141, 1159; (d) R R Kale, V Prasad, V K Tiwari, Lett. Org.



180

Chem., 2010, 7, 136; (e) V Prasad, B B Mishra, R R Kale, D Kumar, V K Tiwari, Org.

Lett., 2012, 14, 2936.

2. (a) D Kushwaha, V K Tiwari, J. Org. Chem., 2013, 78, 8184; (b) KB Mishra, V K Tiwari, J.

Org. Chem., 2014, 79, 5752.

3. (a) D Kumar, A Mishra, B B Mishra, S Bhattacharya, V K Tiwari, J. Org. Chem., 2013, 78,

899; (b) D Kumar, B B Mishra, V K Tiwari, J. Org. Chem.,2014, 79, 251.

IL-17

Efficient synthesis of carbohydrate derived privileged molecules

Chintam, V.V.S. Narayana, Ram Sagar Misra*

Department of Chemistry, School of Natural Science, Shiv Nadar University, Dadri, Greater Noida


The efficientsyntheses of small molecules that specificallyperturb the functions of protein or

enzymes, enable theexploration of biological pathways in cells or organisms.1Further, bioactive

small molecules are widely used to modulateprotein function and can serve as important leads for

drugdiscovery.2 Therefore, the development of an efficient synthesis of a drug-like bioactive small

molecule hasbeen the research focus of medicinal/bioorganic chemists andchemical biologists.3

An efficient diastereoselective one-pot synthesis ofpolycyclic acetal-fused pyrano[3,2-

c]pyrane-5(2H)-one was also achieved through the annulation reaction of 2-C-formylglycals with

various 4-hydroxycoumarins and 4-hydroxy-6-methyl-2H-pyran-2-one. The asymmetric induction

wassignificantly influenced by the C-4 stereogenic center of 2-Cformylglycals. The resulting

polycyclic acetal-fused pyranopyronesdemonstrated anticancer activities.4

Carbasugars are knownfor several biological activities such as antitumor, antiviral, antifungal or

as inhibitors/activators of carbohydrate processing enzymes.5There are several reports where

carbasugars has been used as precursor for synthesizing natural product molecules.6Due to

immense application of carbasugars,many groups in world working on efficient synthesis of these

carbohydrate derivatives.7It is well known that carbasugars are metabolically more stable than

their carbohydrate precursors therefore they are choice for medicinal chemist and chemical

biologist as mimics in living system.8In our moderate effort, we design and develop an efficient

synthetic route for synthesis of six membered carbasugars(Figure 1) mimicking N-acetyl-

glucosamine. N-acetyl glucasamine is a natural ligand for N-acetyl-α-glucosaminidase(NAGLU),

an enzyme responsible for processing the carbohydrates in lysosome.9The details of synthetic

challenges and successful efficient synthesis will be presented therein.



181

OR

NHAcOH

HO

HO

Figure 1.

References

(1) Schreiber, S. L. Bioorg. Med. Chem. 1998, 6, 1127. (2) Schreiber, S. L. Science 2000, 287,

1964. (3) (a) Koehler, A. N.; Shamji, A. F. and Schreiber, S. L. J. Am. Chem Soc. 2003, 125,

8420. (b) Bruke, M. D. and Schreiber, S. L. Angew. Chem.Int. Ed. 2004, 43, 46. (4) Sagar, R.

Park, J. Koh, M. Park, S. B. J. Org. Chem. 2009, 74, 2171-2174. (5) Ernst, B., Magnani, J. L.

Nature Rev. Drug Discov.2009, 661-677. (6) Henrik V.H., Jensen H.H., Liang X., Bols M.,

Chem.Rev. 2002,102, 515-553.

IL-18

Greener and efficient approaches for the syntheses of biologically potent

scaffolds

Devdutt Chaturvedi*

Laboratory of Medicinal Chemistry, Amity Institute of Pharmacy,

Amity University Uttar Pradesh (AUUP), Lucknow Campus, Lucknow-226028, U. P.

E-mails: [email protected], [email protected]

Abstract:

In recent years, development of novel synthetic methodologies have been attracted a great

deal of attention for organic chemists around the globe, for the synthesis of structurally diverse

biologically potent molecules. The advantages associated with these synthetic methodologies are

lesser synthetic steps, use of cheaper and safer new alternatives, involves overall lesser reaction

time, milder reaction conditions, and afforded high yields. Extensive efforts have been made by

organic chemists around the globe and thus developed several kinds of new and highly efficient

methods for the generation of various kinds of structurally diverse molecules of biological

significance.




182

Our group has been working since more than a decade on the development of novel and

efficient methodologies for the synthesis of structurally diverse biologically active compounds. In

the present talk, I would like to emphasize some of our novel and efficient synthetic strategies for

the synthesis of carbamates, dithiocarbamates, xanthates, dialkyl carbonates, S,S-dialkyl

dithiocarbonates, trithiocarbonates, substituted ureas, α-amino nitriles, and substituted N-aryl

lactams etc employing cheap and safe alternatives starting from a variety of starting materials,

reagents and catalytic systems.

References:

(a) Chaturvedi, D. et al. Tetrahedron Lett.2003, 44, 7637-7639; (b) Tetrahedron Lett.2006,

47, 1307-1309; (c) Tetrahedron Lett.2007, 48, 149-151; (d) Tetrahedron Lett. 2007, 48,

5043-5045; (e) Synthesis, 2008, 355-357; (f) Tetrahedron Lett.2008, 49, 4886-4888; (g)

Curr. Org. Chem.,2011, 15, 1593-1624; (h) Tetrahedron Lett.,2012,53, 5398-5401; (i)

Tetrahedron,2012,68, 15-45; (j) Curr. Org. Chem.,2012, 16, 1609-1635; (k) Synlett.,2012,

23, 2627-2630; (l) Org. Biomol. Chem., 2012, 10, 9148-9151; (m) Synlett., 2013, 24, 33-

36.

ORAL

PRESENTATIONS OP-1

Antimicrobial Activity of Synthesized TiO2 Nanoparticles

UPASANA YADAVA, B. C. YADAVB, MANODEEP SENC

aDepartment of Engineering, Amity University, Lucknow-226017, U.P., India

bDepartment of Applied Physics, School for Physical Sciences,

BABASAHEBBHIMRAOAMBEDKAR UNIVERSITY, LUCKNOW-226025, U.P., INDIA

cDepartment of Microbiology, Dr RMLIMS, Lucknow

aEmail: [email protected]


183

ABSTRACT

In recent years, nanotechnology has been flourishing. Nano-structured materials are attracting a

great deal of attention because of their potential for achieving specific processes and selectivity,

especially in biological and pharmaceutical applications. Nanotechnology has become one of the

most practical technologies, because of unique physical and chemical properties of nanomaterials.

Nanomaterials such as TiO2 nanoparticles (TiO2 -NPs), less than 100 nm in diameter, have become

a new generation of advanced materials due to their brilliant and interesting optical, dielectric, and

photo-catalytic characteristics from size quantization. Resistant strains fail to develop if we apply

nanoparticle-based formulations in their media. The antibacterial activities of some nanoparticles,

makes them attractive as a new agents against pathogenic bacteria. Liquid and agar nutrient

medium used for E.coli culture and different antibiotics used for Disk diffusion technique to

evaluate antibiotic resistance pattern of E.coli. Antibacterial effect of 0.01, 0.5, 1 and 1.5% of

nano-TiO2 evaluated via optical density (OD) and Kirby-Bauer disc diffusion test.This strain was

resistant to all antibiotics used in this study. Optical density decrease was observed with nano-

TiO2 concentration increase (0.225, 0.218, 0.158, 0.075, 0.031respectively). Inhibition zone

measurement showed the similar results. The maximum inhibition zone (5mm) was observed in

1.5% of nano-TiO2. Nano materials are known to inactivate cellular enzymes and DNA by binding

to electron-donating groups such as Carboxylates, Amides, Indoles, Hydroxyls, Thiols, and etc.

They cause little pores in bacterial cell walls, leading to increased permeability and cell death.

Based on this study, nano-TiO2 has efficient antibacterial effect and can be used as an antibacterial

agent for different purposes.In recent years, nanotechnology has been flourishing. Nano-structured

materials are attracting a great deal of attention because of their potential for achieving specific

processes and selectivity, especially in biological and pharmaceutical applications.

Nanotechnology has become one of the most practical technologies, because of unique physical

and chemical properties of nanomaterials. Nanomaterials such as TiO2 nanoparticles (TiO2 -NPs),

less than 100 nm in diameter, have become a new generation of advanced materials due to their

brilliant and interesting optical, dielectric, and photo-catalytic characteristics from size

quantization. Resistant strains fail to develop if we apply Nanoparticle-based formulations in their

media. The antibacterial activities of some nanoparticles, makes them attractive as a new agents

against pathogenic bacteria. Liquid and agar nutrient medium used for E.coli culture and different

antibiotics used for Disk diffusion technique to evaluate antibiotic resistance pattern of E.coli.

Antibacterial effect of 0.01, 0.5, 1 and 1.5% of nano-TiO2 evaluated via optical density (OD) and

Kirby-Bauer disc diffusion test.This strain was resistant to all antibiotics used in this study. Optical

density decrease was observed with nano-TiO2 concentration increase (0.225, 0.218, 0.158, 0.075,

0.031respectively). Inhibition zone measurement showed the similar results. The maximum

inhibition zone (5mm) was observed in 1.5% of nano-TiO2. Nano materials are known to inactivate

cellular enzymes and DNA by binding to electron-donating groups such as Carboxylates, Amides,

Indoles, Hydroxyls, Thiols, and etc. They cause little pores in bacterial cell walls, leading to


184

increased permeability and cell death. Based on this study, nano-TiO2 has efficient antibacterial

effect and can be used as an antibacterial agent for different purposes.

OP-2

In-vitro Antibacterial Screening ofAndrographis Paniculata: A Possible

Alternative for Fighting against Mdr Strains

Priti Mathura, Chandni Tandona, Manodeep Senb

aAmity Institute of Biotechnology, Amity University, Uttar Pradesh, Lucknow- 226028

bDepartment of Microbiology, Dr. Ram Manohar Lohia Institute of Medical Sciences, Lucknow

ABSTRACT

The development of bacterial resistance to currently available antibiotics has necessitated distinct

and constant need for safe and efficient therapeutic agents. Plants are considered potent candidate

for this aim. So keeping in view of this, the antibacterial activity of aqueous, ethanol, methanol,

hexane and chloroform extracts ofAndrographis paniculata leaf has been tested in vitro against

Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa. The results of agar well

diffusion assay indicated that all the strains were inhibited by ethanolic extract with greater zone

of inhibition compare to other extracts, while aqueous extract were found to be ineffective against

the tested strains. Our finding suggests that Andrographis paniculata could be a potential source

to develop new efficacious drugs and form a strong basis for further research to isolate novel

compounds from it.

Keywords: Andrographis paniculata, bacterial resistance, agar well diffusion assay.

OP-3

Exploration of Boron Tribromide as C-C bond forming agent

Imran Ahmad, Vinay Pathak, Prema G. Vasudev, Hardesh K. Maurya and Atul Gupta*


185

Central Institute of Medicinal and Aromatic Plants, Lucknow226015E.mail: [email protected],

[email protected]

ABSTRACT

Borontribromide (BBr3) is used as demethylating agent. Current exploration was focused on a new

application of borontribromide as C-C bond forming agent. In this study, borontribromide

mediated C-C bond formation reactions of various cyclic ketons such as chromenone, tetralones,

indanones and thiochromenone were studied. We have observed that methoxy group containing

ketones showed selective C-C bond formation reaction instead of demethylation of methoxy group.

MM2 steric energy calculations for final products showed that reaction favored the formation of

exo or endo cyclic double bond containing products depending upon their low MM2 steric energy

in a specific frame structure as observed in x-ray crystallography. A comprehensive

crystallographic and pi-stacking analysis of products exhibited the formation of enantiomeric

mixture and its centre of inversion was stabilized by a set of three unique pi-pi interactions.

R4 R4

R3X

O X

R3BBr3, DCM

R3X

O

R2

R1 R1

R2

R2

R1

0oC to rtn

OH

O

O

O

OO

O

BBr3

XBBr3

n=1

Demethylation C-C bond formation

R4

R R

R4R3

O

R3

R1

R2

R2

R1

R4

R

BBr3, DCM

0oC to rt

n=0

OP-4

Total Syntheses of Lawsone, Lapachol and β-Lapachone: Pharmacologically

important Naphthoquinones

B. Sathish Kumar, Arvind S. Negi*

Medicinal Chemistry Department, CSIR-Central Institute of Medicinal and Aromatic Plants, P.O.

CIMAP, Kukrail Picnic Spot Road, Lucknow-226015, U.P., India.

E-mail: [email protected] ; [email protected]





186

ABSTRACT

Keywords: napthoquinones, total synthesis, lawsone, lapachol, β-lapachone.

Naphthoquinones are a common sub-structure of many natural products produced as secondary

metabolites [1]. Being an important class of compounds, several partial and total syntheses have

been done. Among these, Lawsone, lapachol and β-lapachone are important biodynamic

naphthoquinones. Lawsone is used for the synthesis of some clinically important anticancer drugs

like atovaquone, dichloroallyllawsone and lapachol. Lapachol underwent clinical trial as cancer

drug candidate by NCI, USA. But dropped due to toxicity concerns [2]. β-Lapachone possesses

potent anticancer activity through induction of DNA Topoisomerase-II mediated DNA cleavage.

β-Lapachone has completed six clinical trials in October 2013, against pancreatic cancer, head and

neck cancer and advanced solid cancer in combination therapy [3].

We report here syntheses of Lawsone (1), Lapachol (2) and β-Lapachone (3) from easily

available starting substrates. All the reaction conditions are simple and straight-forward. The

transformations proceed with overall yields of 57.35%, 26.56%, and 84%. All these reactions can

be upscaled to industrial level.

O

O

OH

O

O

O

OH

O

O

OH

Lawsone

O

Lapachol

-Lapachone

4 steps

11 steps single step

57.34%

26.56% 84%

References

[1] Papageorgiou, V. P. et al. Angew. Chem. Int. Ed.1999, 38, 270-300

[2] Santana, C. F. et al. Rev. Inst. Antibiot.1980, 20, 61-68.

[3] Cragg, G. M. et al. J. Nat. Prod.2014, 77, 703-723.

OP-5

An efficient and novel approach for the syntheses of dithiocarbamates from

their corresponding thiols employing TPP.Br2

Sadaf Zaidi,a,c Amit K. Chaturvedi,c Devdutt Chaturvedi,a,*

aLaboratory of Medicinal Chemistry, Amity Institute of Pharmacy, Amity University Uttar Pradesh

(AUUP), Lucknow Campus, Lucknow-226028, U. P.


187

bDepartment of Chemical Sciences, GLA University, Mathura-281406, U. P.

cDepartment of Chemistry, Amity School of Applied Sciences, Amity University Uttar Pradesh (AUUP),

Lucknow Campus, Lucknow-226028, U. P.

*Corresponding author’s e-mails: [email protected], [email protected]

ABSTRACT

Organic dithiocarbamates have extensively been used as agrochemicals, pharmaceuticals,

intermediates in organic synthesis, protection of amino groups in peptide synthesis, linkers in solid

phase organic synthesis, radical precursors in free-radical chemistry and the synthesis of ionic

liquids. Furthermore, different transition metal complexes of dithiocarbamates have been

synthesized for various studies, primarily because of their applications as organic superconductors.

To satisfy their demand, their synthesis has been changed from the use of costly and toxic

chemicals such as thiophosgene and its derivatives directly or indirectly, to the abundantly

available cheap and safe reagents like CS2. Moreover, their formation by using CS2 employed

harsh reaction conditions such as use of strong bases, higher reaction temperatures and longer

reaction times. Our group has been engaged from past several years for the development of new

methodologies for the preparation of carbamates, dithiocarbamates and related compounds using

cheap, abundantly available, and safe reagents like CO2 and CS2 respectively.a-m In our recent

paper we have reported synthesis of α-amino nitrile employing tri phenylphosphine- -dibromide

(TPP.Br2) as a catalyst and we found that TPP.Br2 is the best catalyst for the synthesis of

dithiocarbamates, employing a variety of reagentsm.In the present paper, we report herein a new

and efficient one-pot method for the synthesis of dithiocarbamates through the reaction of

corresponding thiols with amines employing catalytic amount of TPP.Br2/CS2 system at room

temperature (Scheme 1). To the best of our knowledge, this is the first report for the efficient and

mild synthesis of dithiocarbamates employing TPP.Br2, afforded good to excellent yields (80-

98%).

R1 SH

R2

R3

+ HNR5

R4 Dry DMSO, TPP.Br2, CS2 R1 S

R2

R3

S

NR5

R4

1

Scheme 1

RT , 1-2 hr., 80-98%

References:

(a) D. Chaturvedi,* et al, Tetrahedron Lett.2003, 44, 7637.(c) Tetrahedron Lett.2006, 47, 1307.

(d) Tetrahedron Lett.2007, 48, 149. (e)(f)Tetrahedron Lett. 2007, 48, 5043.; (g)Synthesis2008,

355-357; (h) TetrahedronLett.2008,49, 4886-4888; (i) )Tetrahedron Lett.,2012,53, 5398-5401;(j)




188

Tetrahedron,2012,68, 15-45; (k)Synlett.,2012, 23, 2627-2630; (l) Org. Biomol. Chem.,2012,10,

9148-9151; (m) Synlett.,2013, 24, 33-36

OP-6

Synthesis, characterisation and biological evaluation of some β-lactam

qinazolone derivatives

Krishna Srivastava, Deepa Lakhmani

Department of Chemistry,

Sri Ramswaroop Memorial University, Deva Road Lucknow, Uttar Pradesh, India

ABSTRACT:

The novel series of some β- lactam quinazolone derivatives were synthesised by the reaction of 3-

(p-Arylldenoamino diphenyl )/Aryldeno-amino-2-phenyl-4-(3H) quinazolone, chaloroacertyl

chloride and tri ethyl amine in 1:1 ratio. The newly synthesised compounds are screened for their

biological evaluation with general characterisation by elemental analysis FITR, 1H NMR, 13C

NMR and mass spectroscopy. Derivatives showed higher to moderate activity against different

pathogenic microbial strain.

Keywords- Quanzolone chloroacetyl chloride, triethylamine, antharanilic acid, 1,1 biphenyl-

4,4-diamine and Aeromatic aldehyde, glacial acetic acid.

OP-7

Synthesis of Triazine cored-Sulfone Terminated Dendrimers

Shaziya Khanam, Ranjana S. Khanna, Ashish Kumar Tewari*

Department of Chemistry (Centre of Advanced study), Faculty of Science, Banaras Hindu University,

Varanasi-221005.

[email protected]

ABSTRACT

Synthetic aspects of dendrimers with unique physical and chemical properties are attracting great attention

among scientists in many disciplines including light harvesting,drug delivery, biomedical, catalysis and

material applications. Sulfonimide, triazoles and triazine were found to exhibit essential biological activities

such as anti-HIV, antibacterial and antiallergic properties . Till now, several kinds of dendrimers have been

synthesized. . In this context, we have incorporated triazole and triazine unit into sulfonimide-based


189

dendrimer system and developed an efficient andpreparatively simple convergent synthetic methodology

for the synthesis of different denrimers via click chemistry with high purity and excellent yield. -

S. M. Grayson, J. M. J. Frechet, Chem. Rev. 2001, 101, 3819−3867.

A) R. C. Ogden and C. W. Flexner, Eds., Protease Inhibitors in AIDS Therapy (Marcel

Dekker, New York, 2001). (B) C. T. Supuran and A. Scozzafava,Exp. Opin. Ther. Patents,10, 575

(2000).(C) C. T. Supuran and A. Scozzafava,Curr. Med. Chem. Immunol. Endoc.Metab. Agents,1,61

(2001).

S. C. Zimmerman, W. F. Zeng, D. E. C. Reichert, Kolotuchin, S. V. Science 1996, 271, 1095-1098.

S. C. Zimmerman, W. F. Zeng, D. E. C. Reichert, Kolotuchin, S. V. Science 1996, 271, 1095-1098.

C.Y. Lee, R. Held, A. Sharma, R. Baral, C. Nanah, D. Dumas, S. Jenkins, S. Upadhaya, W. Du, J. Org.

Chem.2013, 78, 11221−11228.

OP-8

An efficient method for the synthesis of substituted-1,3-oxazolidine-2,4-diones

through the corresponding tosyloamides using Triton-B/CO2 system Amit K. Chaturvedi,a,b Devdutt Chaturvedi,*,c and Virendra Mishraa

aSynthetic Research Laboratory, Department of Chemistry, B. S. A. P. G. College, Mathura-281004, U. P.,

India

bDepartment of Chemical Sciences, GLA University, Mathura-281406, U. P

cLaboratory of Medicinal Chemistry, Amity Institute of Pharmacy, Amity University Uttar Pradesh


ABSTRACT


190

Substituted 1,3-oxazolidine-2,4-diones are biologically active compounds which finds use as

anti-convulsants, particularly interesting therapeutic properties were found in trimethadione

(3,5,5-trimethyl oxazolidine-2,4-diones), paramethadione (5-ethyl-3,5-dimethyl oxazolidine-2,4

diones) and malidone (3-allyl-5-methyl oxazolidine-2,4-dione). Several compounds belonging to

this class have displayed remarkable herbicidal activity. These compounds have been found as

useful synthon for the synthesis of biologically potent derivatives such as substituted α-

hydroxycarboxamides, substituted α-hydroxyhydrazidesetc. Their traditional syntheses involved

the use of harmful reagents such phosgene, its derivatives and carbon monoxide or isocyanates.

Recently, carbon dioxide has only been used as a cheap and safe alternative in the synthesis of

substituted 1,3-oxazolidine-2,4-diones employing the electrochemical form of carbon dioxide

using various kinds of starting materials and reagents/catalytic systems. Moreover, their formation

using CO2 employed harsh reaction conditions such as higher reaction temperatures, longer

reaction time and tedious workup. Therefore, we would like to embark on the developments of

improved procedures for the synthesis of substituted 1,3-oxazolidine-2,4-diones employing

gaseous carbon dioxide as a source of carbonyl functionality. Our group has been engaged over

several years on the development of new and efficient and safer protocols for the synthesis of

carbamates, dithiocarbamates, dithiocarbonates (xanthates) using cheap and abundantly avaliable

reagent like CO2 and CS2 respectively. In the present paper, various kind of substituted-1,3-

oxazolidine-2,4-diones Ihave been synthesized through their corresponding tosyloamides

employing Triton-B/CO2 System (Scheme 1).

O

OR1

NHR3

O

Tos

R1

NO

Dry DMSO, Triton-B

R3

X = leaving group, i.e. tosylates

R1 = R2 = alkyl/aryl/ heteroaryl and its substituted derivatives

R2

CO2, 60oC, 2-3.5h

Substituted tosyloamides

R3 = alkyl/aryl/cycloalkyl/naphthyl/substituted aryl/heteroaryl

R2

80-98%

123

1

2

3

45

I

Scheme 1

Poster

Presentations


191

PP-1

Nephroprotective potential of Trichosanthes dioica R. leaves extract against

Cisplatin induced Nephropathy in albinos

Ramesh Kumar Guptaa’b*, Sudhansu Ranjan Swaina, Padala Narasimha Murthyb, Jagannath Sahooc

aSherwood College of Pharmacy, Barabanki -225001, Uttar Pradesh, India.

b Royal College of Pharmacy and Health Sciences, Berhampur -760002, Orissa, India.

cDepartmentof Pharmaceutics, S. R. M. S. College of Engineering and Technology, Bareilly

Uttar Pradesh 243202, India.

ABSTRACT

Leaves and fruits ofTrichosanthes dioicaR.used for treatment of jaundice, oedema, alopecia,

enlargement of liver and spleen.

Objective: To evaluate nephroprotective potential ofTrichosanthes dioicaleaves extract against

cisplatin induced nephrotoxicity.

Methodology: The animals were divided into four groups containing six animals in each group.

Group1 served as control and received normal saline throughout the experiment, Group II (Modal

Control) received single dose of cisplatin (5mg/kg i.p.), 1st days, Group III (Protective) received

TLE extract (200mg /kg p.o.) for 1st to 10th day and 11th day, single dose (5mg/kg, i.p.) of cisplatin

was administered, Group IV (Curative) received same dose of cisplatin on day 1st, and after 6th

days TLE extract (400mg / kg p.o.) was administered up to 16th days. Plasma and urine urea and

creatinine, kidney weight, urine output, blood urea nitrogen, urinary sodium and potassium level,

renal enzymatic and non-enzymatic antioxidants and LPO was evaluated in various experimental

groups of rats.

Results: It was observed that the cisplatin treatment induced significant elevation in plasma and

urine urea, creatinine, kidney weight, blood urea nitrogen, plasma Na+ and K+ level, renal LPO

along with significant decrement in urine output, renal enzymatic and non-enzymatic antioxidants.

TLE 200 and 400 mg/kg treatment to cisplatin treated rats’ recorded significant decrement in

plasma and urinary parameters along with significant increment in renal enzymatic and non-

enzymatic antioxidants.

http://www.srmscet.edu/

https://www.google.co.in/url?sa=t&rct=j&q=&esrc=s&source=web&cd=2&cad=rja&uact=8&ved=0CCMQjBAwAQ&url=http%3A%2F%2Fwww.srmscet.edu%2FCET%2Findex.aspx&ei=XumOVKWDN8SLuASjq4LADQ&usg=AFQjCNEf_NXl51JX2cN8ZQclzh_HiHT20A&sig2=ljtESz-W1DO-tsoxFrGugQ


192

Conclusion:These finding powerfully supports that Trichosanthes dioicaleaves extract acts in the

kidney as a potent scavenger of free radicals to prevent the toxic effects ofcisplatin induced renal

toxicity.

Keywords: Nephrotoxicity, Cisplatin.

PP-2

Multidimensional Potential of Substituted Benzoxazole Containing Molecule in

Functional Materials

Arun Kumar, Anup K. Sirbaiya, Kuldeep Singh

Faculty of Pharmacy, Integral University Kursi Road, Lucknow, 226026, Uttar Pradesh, India

*Address for Correspondence:-

E-mail ID: [email protected]

ABSTRACT

In recent years heterocyclic compounds analogues and derivatives have attracted wide attention

due to their useful biological and pharmacological properties. Benzoxazole is among the usually

occurring heterocyclic nuclei in many marine as well as natural plant products. The small and

simple benzoxazole nucleus possesses numerous pharmacological activities like- antitumor,

antimicrobial, antileishmanial, anti-inflammatory, anticancer, anticonvulsant, HIV protease

inhibitor and antidiabetic activities. Since, a wide range of methods have been reported for the

preparation of these heterocyclic compounds including the condensation of carboxylic acids,

orthoesters, acid chlorides, nitriles amides, aldehydes and esters with o-substituted amino

aromatics derivatives from orthoesters. 2-amino phenyl or 5-amino (p-substituted phenyl)

benzoxazoles were obtained by heating substituted benzoic acid with 2-4-diamino phenol in PPA

(polyphosphoric acid). rapid and efficient condensation of 2-amino phenol with various aldehyde

were carried out using I2 in solvent free condition with or without microwave irradiation to afford

corresponding 2-substituted benzoxazole in maximum yield. Benzoxazole have been synthesized

in non-polar high boiling solvent such as toluene and xylene in model reaction addition amino



193

phenol react with acid chloride in present of base. The present review focuses on the different kind

of reactions involved in synthesis as well as cyclization of benzoxazole nucleus and its derivatives.

Keywords: - Benzoxazole, Antitumor, Antimicrobial, Anti convulsant activity.

PP-3

In-Silico Analysis to Access the Antibacterial Effect of Schiff Bases of

Fluoroquinolones: Molecular Docking Approach

Anup K. Sirbaiya, Arun Kumar, Stuti Verma, Satya P. Singh, Vaseem A. Ansari

Faculty of Pharmacy, Integral University, Dasauli, Kursi Road Lucknow-226026

ABSTRACT

Docking studies of synthesized compounds were performed by Autodock version 1.5.4 suit and

Cygwin interface was used in the Microsoft Windows 7 professional Version 2008, Service pack

3 operating System on Intel (R) i5 (TM), CPU @ 3.30 GHz and 8.0 GB of RAM of Intex Machine.

We implemented molecular docking methods followed by the searching the best conformation of

enzymes and carcinogens complex on the basis of binding energy. Water molecules were removed

from the protein structures before docking and hydrogen atoms were added to all target proteins.

Kollman united charges and salvation parameters were added to the proteins. Gasteiger charge was

added to the ligands. Grid box was set to cover the maximum part of proteins and ligand.

The Molecular docking simulation study ofMycobacterium tuberculosis DNA Gyrase Type-A,

PDB ID- 4G3N as a macromolecule with Test Compounds as a ligands was performed by the use

of AutoDock 1.5.4, in this study we found that Test Compounds are binding with the

Mycobacterium Tuberculosis DNA Gyrase Type-A, very efficiently as compare to exciting drug.

Keywords: In- Silico Analysis, Molecular Docking, Mycobacterium tuberculosis, Autodock.

PP-4

Green Chemistry: Solvents in the Pharmaceutical Industry

Mehnaz Kamal1, Talha Jawaid2, Md. Azizur Rahman1, Mohd.Mujahid1, Ranjan Kumar1, Arun Kumar1,

Kuldeep Singh1

1Faculty of Pharmacy, Integral University, Dasauli, Kursi Road, Lucknow (U. P.), India

2Hygia Institute of Pharmaceutical Education and Research, Ghaila road, Lucknow (U. P.), India

*E-mail: [email protected]


194

ABSTRACT

Green chemistry expresses an area of research developing from scientific discoveries about

pollution awareness and it utilizes a set of principles that reduces or eliminates the use or

generation of hazardous substances in all steps of particular synthesis or process. Chemists and

medicinal scientists can greatly reduce the risk to human health and the environment by following

all the twelve valuable principles of green chemistry proposed by Anastas and Warner. The

selection and use of solvents is emphasized as regards methods to minimize environmental impact.

Case studies of successful process development to achieve improved green processes are included.

Keywords: Green chemistry; Pharmaceuticals; Solvents; Case studies.

PP-5

Future Prospects of Cough Treatment: Herbal Medicines V/S Modern Drugs

Tarique Mahmood, Yasmeen Jahan, Arun Kumar and Paramdeep Bagga

Faculty of Pharmacy, Integral University, Lucknow

Email.ID [email protected]

ABSTRACT

Drugs currently used to treat cough are among the most widely used over-the-counter drugs in the

world, a recent analysis suggest that there is a little evidence to support such drugs produce any

meaningful efficacy . The primary action of currently available cough suppressants is on the central

cough pathway. This causes significant side effects and limits their use. There is a current huge

unmet need for the development of safe, effective antitussive therapeutic options in the treatment

of persistent cough as alternative to existing medications that why complimentary alternative

medicine therapies continue to gain popularity as modalities for the treatment of cough. Present

study comprises the collective information on all herbal antitussive, mucolytics and expectorant

plants reported in traditional systems as well as the polyherbal formulations used in practice for

cough ailments like Joshina, Koflet, D'cold and Kafbin. This study concludes with the comparative

evaluation of these herbal drugs with modern medications used in clinical practice in terms of

safety, efficacy and clinical status.



195

Keywords: Cough, Herbal antitussive, cough formulations, expectorant plants.

PP-6

Aldose Reductase Inhibitor fidarestats: A Promising Drug Target In

autophagy-Mediated Colorectal Cancer

Saumya Pandey1, 2M.Sc. (Biochemistry), Ph.D. (Life Science)

1Research Cell, Department of Research,

Amity University Uttar Pradesh, Lucknow, UP, India

2Department of Biochemistry & Molecular Biology,

University of Texas Medical Branch, Galveston, TX, USA

ABSTRACT:

Colorectal cancer (CRC) is a major public health problem. Aldose reductase (AR) catalyzes the

rate limiting step of polyol pathway of glucose metabolism; besides reducing glucose to sorbitol,

AR reduces lipid peroxidation-derived aldehydes/glutathione conjugates. Novel AR Inhibitor

(ARI) Fidarestat is emerging as a potent drug target in inflammatory diseases (1, 2). To investigate

the potential role of AR inhibition using Fidarestat in the regulation of cell death in CRC.Glucose

depletion (GD) was used as “physiological trigger” for cell death; HT-29 and SW480 CRC cells

were rinsed with glucose-free RPMI-1640, followed by incubation in GD medium +/- Fidarestat,

protein extraction/estimation and western blot. Microtubule associated protein light chain (LC)3,

autophagy-related gene (ATG)5, ATG7 and Beclin1proteins were expressed in GD-conditioned

CRC cells +/- Fidarestat (10 µM); LC3II (14 kDa) expression was relatively higher compared to

LC3I isoform. High mobility group box (HMG)1 and Bcl-2 expression(s) were relatively low;

GAPDH was used as internal reference. GD +/- ARI induced autophagy in HT-29 and SW480

cells, thereby implicating Fidarestat as a promising therapeutic target in CRC; future studies with

more potent ARIs are warranted to provide innovative pharmacological strategies for drug

development and cancer therapy in patients.

References:

1.Pandey S, Srivastava SK, Ramana KV. A potential therapeutic role for aldose reductase

inhibitors in the treatment of endotoxin-related inflammatory diseases. Expert OpinInvestig Drugs

2012; 21:329-39.

2.Pandey S, Chandravati. Autophagy in cervical cancer: an emerging therapeutic target.Asian Pac

J Cancer Prev 2012; 13:4867-71.

Key words: Aldose reductase; Autophagy; Colorectal cancer; Drug; Fidarestat

http://www.ncbi.nlm.nih.gov/pubmed?term=Pandey%20S%5BAuthor%5D&cauthor=true&cauthor_uid=22283786

http://www.ncbi.nlm.nih.gov/pubmed?term=Srivastava%20SK%5BAuthor%5D&cauthor=true&cauthor_uid=22283786

http://www.ncbi.nlm.nih.gov/pubmed?term=Ramana%20KV%5BAuthor%5D&cauthor=true&cauthor_uid=22283786

http://www.ncbi.nlm.nih.gov/pubmed/23244072


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PP-7

Recent Advances of Functionalized 2-Aminobenzothiazole Scaffolds

Arun Kumar,Param Deep Bagga, Tarique Mahmood, Yasmeen Jahan, Mehnaz Kamal

Faculty of Pharmacy, Integral University Kursi Road, Lucknow, 226026, Uttar Pradesh, India

E-mail ID: [email protected]

ABSTRACT

The attractiveness of heterocyclic compounds in medicinal chemistry has increased significantly

in the past few decades as they have been proven to be highly active for a number of purposes.

More specifically, 2-Aminobenzothiazole and its derivatives is a versatile fused heterocyclic

scaffold with extensive pharmaceutical applications. Several 2-aminobenzothiazole derivatives

show a variety of pharmacological properties like anticancer, antibacterial, antifungal, anti-

inflammatory, analgesic, anti-HIV, antioxidant, anticonvulsant, antitubercular,

antidiabetic,antileishmanial, antihistaminic, antimalarial and other medicinal agents. The broad

spectrum of pharmacological activity in substituted 2-Aminobenzothiazole derivative indicates

that, this series of compounds is of an undoubted interest. Some of the compounds containing 2-

aminobenzothiazole ring system are in clinical usage for the treatment of various

diseases/disorders. Herein, we review the recent developments covering the past few years

concerning the advancements in synthetic methodology for the preparation of medicinally relevant

2-aminobenzothiazole-containing heterocyclic structures.

Keywords: - 2-aminobenzothiazole, Antitumor, Antimicrobial, Anti convulsant activity.

PP-8

Antistress Potential of Some Indian Medicinal Plants

Aleza Rizvi, Anuradha Mishra, Mohd. Ahmad

Faculty of Pharmacy, Integral University, Lucknow, India

ABSTRACT



197

Stress is a normal part of everyday life .It has been defined as the pattern of physiological reactions

that prepares an organism for action. If the stress is extreme, the homeostatic mechanism of an

organism become deficit and the survival becomes threatened. It modulates the activities of the

body’s systems, adversely affecting their functioning to maintain health .Scientists in this growing

field have discovered that it modulates the activities of the nervous, endocrine, and immune

systems. Mind-body medicine is developing unconventional methods for coping with stress-

related disorders. Drugs used for mind-body therapies that have been found to help reduce stress,

and consequently, treat stress-related disorders are known as anti stress drugs.

All allopathic drugs usually have side effects. Herbal anti-stress products have the advantage of

the limited side effects. Medicinal plants have been known for millennia and are highly esteemed

all over the world as a rich source of therapeutic agents for the prevention of stress related diseases

like cancers, coronary disease, and some autoimmune diseases . Some herbal drugs to reduce stress

are mandarin (Citrus Nobilis), sweet orange (Citrus aurantium), bergamot (Citris bergamia),

clary sage (Salvia sclarea), grapefruit (Citrus paradisi), lemon (Citrus limonum), lime (Citrus

aurantifolia), basil (Ocimum basilicum), lavender (Lavendula offinialis), etc.

Nature has bestowed our country with an enormous wealth of medicinal plants; therefore India has

often been referred to as the Medicinal Garden of the world. The aim of this review is to highlight

the plants which containing anti-stress activity from preclinical and clinical evaluations including

ayurvedic origin.

Keywords: Anti-stress, Medicinal plants, Ayurveda.

PP-9

Quality Assurance in Herbal Medication

Doli R. Das and Anupam Kr. Sachan

Dayanand Dinanath College, Institute of Pharmacy, Kanpur-209214

ABSTRACT

Herbal medicine, beginning its exponential growth in the last few decades and is getting

popularized in developing as well as in developed countries owing to its natural origin and less

significant side effect. The efficacy and safety of any pharmaceutical product is determined by the

compounds which it contains. The purpose of quality control is to ensure that each dosage unit of

the drug product delivers the same amount of active ingredients and is, as far as possible, free of

impurities. As herbal medicinal products are complex mixtures which originate from biological


198

sources, great efforts are necessary to guarantee a constant and adequate quality. By carefully

selecting the plant material and a standardized manufacturing process the pattern and concentration

of constituents of herbal medicinal products should be kept as constant as possible as this is a

prerequisite for reproducible therapeutic results. This grow in the use of herbal product has also

given rise to various forms of exploitation and adulteration of the products leading to consumer’s

and manufacturer’s dissatisfaction and in some instances serious consequences. Quality control

for the efficacy and safety of herbal products is fundamental. The quality of herbal medicine

explicitly; the summary of the constituents in the final product has implications in efficacy and

safety. Compared with Synthetic drugs, the criteria and the approach for herbal drugs are much

more complex. Some of the parameters including macro and microscopic examination, extractive

values, foreign organic matter, ash values, chromatographic examination, qualitative chemical

evaluation, toxicological studies, etc will eliminate all problems in quality control of herbal

formulations to obtain better formulations.

Keywords: Herbal Medicine, Quality, Efficacy, Safety

PP-10

Various Polyhedral Formulations Used for the Treatment of Type 2 Diabetes

Mellitus

Talha Jawaid1, Mehnaz Kamal2, Shoea1, Pooja1, Braj Nandan Verma1

1Department of Pharmacology, Hygia Institute of Pharmaceutical Education and Research, Ghaila Road,

Lucknow, U. P., India

2Faculty of Pharmacy, Integral University, Kursi Road, Lucknow, U. P., India

ABSTRACT

Diabetes Mellitus is a chronic widely spread human disease. Diabetes mellitus (DM), both insulin-

dependent DM (IDDM) and non-insulin dependent DM (NIDDM) is a common and serious

metabolic disorder throughout the world. Search for an effective drug, alone or in combination,

for treatment of diabetes still remain elusive. Herbal formulations used extensively in traditional

systems of medicine may provide a suitable alternative for this. Traditional plant treatments have

been used throughout the world for the therapy of diabetes mellitus. In spite of all the advances in

therapeutics, diabetes still remains a major cause of morbidity and mortality in the world. Herbal

formulations are becoming popular now days particularly in the treatment of Type 2 diabetes.


199

Though there are various approaches to reduce the ill effects of diabetes and its secondary

complications, herbal formulations are preferred due to lesser side effects and low cost. This

review focuses on the potential of different polyherbal formulation in the treatment of diabetes.

Keywords: Type 2 diabetes; Antidiabetic activity; Aurvedic polyherbal formulations.

PP-11

Efficient Synthesis of N-Acetyl Glucosamine derived Carbasugar analogous for

Biological Application

Chintam V.V.S. Narayana, Ram Sagar*

Department of Chemistry, School of Natural Sciences, Shiv Nadar University,

Dadri, Greater Noida 201314, Email:[email protected]

ABSTRACT

Carbasugars are known for several biological activities such as antitumor, antiviral, antifungal or

as inhibitors/activators of carbohydrate processing enzymes.1There are several reports where

carbasugars has been used as precursor for synthesizing natural product molecules.1Due to

immense application of carbasugars, many groups in world working on efficient synthesis of these

carbohydrate derivatives.2In our moderate effort, we design and develop an efficient synthetic

route for synthesis of six-membered carbasugars mimicking N-acetyl-glucosamine. N-acetyl

glucasamine is a natural ligand for N-acetyl-α-glucosaminidase (NAGLU), an enzyme responsible

for processing the carbohydrates in lysosome.3 It is well known that carbasugars are metabolically

more stable than their carbohydrate precursors therefore they are choice for medicinal chemist and

chemical biologist as mimics in living system.4 We design an efficient synthetic route for

carbasugars analogues based on core structure shown in figure 1. The details of synthetic

challenges and successful efficient synthesis will be presented in poster therein.

OR

OH

HO

HO

NHAc

Figure 1. Core structure of carbasugar

References:

1. J.Duchek, D.R..Adams, and T.Hudlicky, Chem.Rev., 111, 2011,4223.



200

2. Odo´nArjona,Ana M. Go´mez, J. Cristo´balLo´pez, and Joaquı´nPlumet, Chem.Rev.107,

2007,1919-2036.

3.ElizebathFicko-Blean, Keith A Stubbs, A.B.Borston.Proc. Natl. Acad. Sci. U.S.A., 105,2008,

6560.

PP-12

Ultrasonic Contrast Physics of Microbubbles

Kirti Bhatia

Amity University, Lucknow Campus, Lucknow

[email protected]

ABSTRACT:

Gas filled microbubbles are known as ultrasound contrast agents for medical ultrasound imaging

and for non-invasive drug delivery to different tissues. Ultrasound radiation are used which are

non hazardous. Today imaging with ultrasound in combination with microbubbles is preferred

compared to other diagnostic techniques for low cost and rapidity. The ultrasonic field can be

focused at the target tissues and organs; thus, selectivity of the treatment can be improved, reducing

undesirable side effects. This review focuses on the characteristics of microbubbles that give them

therapeutic properties as well and some important aspects of ultrasound parameters that are known

to influence microbubble-mediated drug delivery. In addition, current studies on novel

therapeutical application of microbubbles are also discussed.

PP-13

Synthesis and Biological Activities of Some Substituted Pyran Derivatives

Jaya Pandey

Amity School of Applied Sciences, Amity University, Uttar Pradesh, Lucknow Campus





201

ABSTRACT

Fused carbocyclic and heterocyclic fused ring systems constitute an important class of natural

products with immense pharmacological properties. The biological importance of pyrans as an

anticoagulant, aflatoxins as mycotoxins and of coumestrol as an estrogen and a phytoalexin have

led to a considerable amount of work in the field of fused ring systems. Recently, the

dibenzopyranone/pyrans and naphthopyran nucleus have surfaced as common ring system of a

group of antibiotics, antibacterials, antitumors and immunomodulators, etc. exemplified by

alternariol, ravidomycin, shilajit, ellagic acid etc. Several carbocyclic and heterocyclic compounds

have recently been reported in literature such as KCA-098, LY-356156, and coumestrol analogue

etc. which selectively modulate the activity of estrogen receptor (ER) showing complete antagonist

effect at breast and uterus yet retain the positive effect on central nervous, cardiovascular and

skeletal systems. These compounds termed as 'selective estrogen receptor modulators (SERMs)'

cause increase in bone mineral density (BMD), reduce serum cholesterol level and are completely

antagonists to breast and uterus tissues, therefore, are being evolved as antiosteoporotic agents.

Our continuing effort on the development of 2,3-diarylbenzopyrans as selective estrogen receptor

modulators led us to synthesize some dibenzopyranone/pyran molecules and they were evaluated

for anti-implantation, estrogenic, anti-estrogenic and anti-osteoporotic activities. Synthesis and the

results of biological activities of these molecules will be presented.

References

1. Pandey, J.; Hajela, K. “Synthesis and biological activities of some substituted 6H-dibenzo

[b,d] pyran-6-one and 6,6-dimethyl 6H-dibenzo [b,d] pyran derivatives” 2014 ( US)Global

Journal of Science Frontier Research (GJSFR)ISSN NO: Online: 2249-4626 Print:

Chemistry, B,0975-5896

2. Pandey, J.; Hajela, K.; Dwivedi, A. “Studies on the Synthesis and Biological Efficacy of

Some New 6H-Dibenzo [b,d] pyran-6-one and 6,6-dimethyl dibenzopyrans as Estrogen

Antagonists/Modulators.” Bioorg. Med. Chem.2004, 12, 2239-2242.

3.

PP-14

Role of Natural Polymers in Drug Delivery

Richa, Nimisha and Smriti

Department of Chemistry, Amity School of Applied Sciences,

Amity University Uttar Pradesh, Lucknow Campus, Lucknow-226028, U. P.


202

Abstract:

Natural polymers are having important role in the field of drug delivery. The polymers can be

utilized in the process of drug delivery. It involves in the field of art, science and technology.

Natural polymers are biogenic, recognized by the body as analogous to the polymers in the

biological system and thus making them suitable in formulations of drug delivery systems. In

addition, their biological properties such as cell interactions, enzyme facilitated degradation and

similarity to the extracellular matrix; and their chemical malleability make natural polymers prime

materials for drug delivery applications. Mainly this research topic focuses on the processes and

applications of natural polymers in drug delivery.

Key words: Natural polymers, drug delivery, extracellular matrix.

PP-15

Synthesis of novel substituted 4- Thiazolidinones derivatives

Desh Deepak Pandey and Ashutosh Pathak

Rameshwarm Institute of Technology & Management Lucknow

ABSTRACT

In the present research work a series of novel substituted 4- Thiazolidinones adducts were

synthesized using three step reaction procedure starting from orthophenylenediamine. And this

synthesis was carried by both Conventional and microwave irradiation synthesis. The structures

of all compounds have been confirmed by physical and spectral analysis (IR, 1H NMR and FAB

Mass). Microwave method is used for carrying out chemical transformations which are pollution

free and eco-friendly. There are numerous biologically active molecules with five membered rings,

containing two hetero atoms. 4-Thiazolidinones and their derivatives belong to such an important

class of compounds. It is well known that benzimidazoles possess various activities like

antimicrobial, analgesic, Antioxidant and anti-inflammatory. 4-Thiazolidinones are also exhibit a

plethora of biological activities such as analgesic, antibacterial, antifungal, anti-inflammatory,

antimicrobial, antidiabetic, antioxidant etc. As the clubbing of 2-substituted benzimidazole and 4-

thiazolidine leading to a new molecule which lacks carboxylic group may have improved activity

with less or no gastric effects.2

Keywords: Thiazolidinone, Benzimidazole, Microwave Irradiation Synthesis, Thioglycolic acid.


203

PP-16

Effect of Cichorium Intybus Leaves on N-Nitrosodiethylamine Induced Hepatotoxicity in Wistar

Rats

Neha Mathur 1, Deepshikha Pande Katare2, Vidhu Aeri3

1 Amity Institute of Pharmacy, Amity University Uttar Pradesh, Lucknow, India.

2 Amity Institute of Biotechnology, Amity University Uttar Pradesh, Noida, India.

3 Department of Pharmacognosy & Phytochemistry, Faculty of Pharmacy, Jamia Hamdard

University, New Delhi, India.

ABSTRACT

Cichorium intybus (Asteraceae) is used as traditional medicine in India for various liver related

disorders. The present study evaluates the hepatoprotective potential of leaf extract on N-

nitrosodiethylamine induced hepatotoxicity, which is commonly present in foods, beverages,

tobacco smoke, herbicides, pesticides, drinking water, and industrial pollution. The leaves were

sorted as per their size (short, medium, large) and subjected to extraction with ethanol, water and

ethanol: water (1:1 w/w) by cold maceration and hot soxlation.The extract having the highest

extractive value 80.7%w/w was selected for animal studies. Group I, II, III, served as control, toxic

and standard. Group IV and V were post treatment receiving 400 mg/kg body weight and 800

mg/kg body weight respectively and group VI as pre treatment group receiving 800 mg/kg body

weight of the extract before the induction of toxicity.The level of serum markers such as aspartate

aminotransferase (AST), alanine aminotransferase (ALT), alkaline phosphatase (ALP) were

significantly suppressed (P<0.0001) in both the groups receiving 400 mg/kg body weight and 800

mg/kg body weight of extract as compared to the toxic group. Activities of enzymic (superoxide

dismutase (SOD), catalase (CAT), glutathione peroxidase (GPx), glutathione-S-transferase (GST),

and glutathione reductase (GR)) antioxidants were significantly increased (P<0.05) on

supplementation with the extract. Histopathological studies also evidenced the liver protective

effect of the plant extract. The study results show that treatment with 800 mg/kg body weight

Cichorium intybus extract before or after NDEA provides protection against the hepatotoxicity

caused by NDEA.


204

PP-17

DESIGN AND SYNTHESIS OF NOVEL SAPONINS ENCOMPASSING TRI AND

TETRASACCHARIDE AS VACCINE ADJUVANTS

DEBABRATA BHUNIA, VEERJALA NAVEEN KUMAR AND H. M SAMPATH KUMAR

Vaccine Immunology Laboratory, Natural Products Chemistry Division, Indian Institute of Chemical

Technology, Hyderabad-500 007, IndiaEmail: [email protected],

ABSTRACT

Saponins are natural or synthetic molecules with soap like characteristic bearing one or more

hydrophilic glycoside moieties linked to triterpenoid lipid head group. Owing to their amphipathic

nature, they act as powerful vaccine delivery systems and best example is QS21-a saponin with

complex structure isolated form Quillaja bark which is clinically approved as vaccine adjuvant. In

view of their efficacy in vaccine delivery vehicles, we designed saponins bearing tri and

tetrasaccharide cluster linked to cholesterol unit across a spacer of variable length. A focused

library of novel saponins thus designed has been subjected to various immunological evaluations

to determine their adjuvanticity and significant Th1 activation has been observed when the

compounds were tested in vivo for their immunogenicity on ova sensitized splenocytes. The

design, synthesis and immunological studies of novel synthetic saponins shall be presented.

1. Soltysik S, Wu JY, Recchia J, Wheeler DA, Newman MJ, Coughlin RT, Kensil CR.

Vaccine. 1995; 13(15):1403-10.

2. Estrada A, Katselis GS, Laarveld B, Barl B. Comparative immunology, microbiology and

infectious diseases. 2000; 23(1); 27-43

3. a) H M Sampath Kumar, Parvinder Pal Singh, Naveed A Qazi, Jada Srinivas, Fayaz Malik,

TabasumSidiq, Amit Gupta, AnamikaKhajuria, K A Suri, N K Satti, G N Qazi, Vaccine

12/2010; 28(52):8327-37; b) Parvinder Pal Singh, Naveed Ahmed Qazi, Syed Shafi, D

Mahendhar Reddy, Abid H Banday, P Bhaskar Reddy, K A Suri, B D Gupta, N K Satti,

Basant P Wakhloo, H M Sampath Kumar, G N Qazi; Journal of Molecular Catalysis B

Enzymatic 01/2009; 56:46-54. c) P. Singh, Debabrata Bhunia, Yogesh K Verma, Tabasum

Sidiq, Anamika Khajuria, Amit Gupta, M Preethi Pallavi, S Surya Vamshi, Gulam N Qazi,

Halmuthur M Sampath Kumar; International immunopharmacology 593-600/17/2013


http://www.ncbi.nlm.nih.gov/pubmed?term=Soltysik%20S%5BAuthor%5D&cauthor=true&cauthor_uid=8578817

http://www.ncbi.nlm.nih.gov/pubmed?term=Wu%20JY%5BAuthor%5D&cauthor=true&cauthor_uid=8578817

http://www.ncbi.nlm.nih.gov/pubmed?term=Recchia%20J%5BAuthor%5D&cauthor=true&cauthor_uid=8578817

http://www.ncbi.nlm.nih.gov/pubmed?term=Wheeler%20DA%5BAuthor%5D&cauthor=true&cauthor_uid=8578817

http://www.ncbi.nlm.nih.gov/pubmed?term=Newman%20MJ%5BAuthor%5D&cauthor=true&cauthor_uid=8578817

http://www.ncbi.nlm.nih.gov/pubmed?term=Coughlin%20RT%5BAuthor%5D&cauthor=true&cauthor_uid=8578817

http://www.ncbi.nlm.nih.gov/pubmed?term=Kensil%20CR%5BAuthor%5D&cauthor=true&cauthor_uid=8578817

http://www.ncbi.nlm.nih.gov/pubmed/8578817

http://www.researchgate.net/researcher/14176149_H_M_Sampath_Kumar/

http://www.researchgate.net/researcher/57923565_Parvinder_Pal_Singh/

http://www.researchgate.net/researcher/48407152_Naveed_A_Qazi/

http://www.researchgate.net/researcher/57845409_Jada_Srinivas/

http://www.researchgate.net/researcher/39435238_Fayaz_Malik/

http://www.researchgate.net/researcher/50493468_Tabasum_Sidiq/

http://www.researchgate.net/researcher/40001484_Amit_Gupta/

http://www.researchgate.net/researcher/39772388_Anamika_Khajuria/

http://www.researchgate.net/researcher/39665328_K_A_Suri/

http://www.researchgate.net/researcher/39814538_N_K_Satti/

http://www.researchgate.net/researcher/39783788_G_N_Qazi/

http://www.researchgate.net/journal/1873-2518_Vaccine


http://www.researchgate.net/researcher/48407152_Naveed_Ahmed_Qazi/

http://www.researchgate.net/researcher/32690538_Syed_Shafi/

http://www.researchgate.net/researcher/81025155_D_Mahendhar_Reddy/

http://www.researchgate.net/researcher/81025155_D_Mahendhar_Reddy/

http://www.researchgate.net/researcher/28261143_Abid_H_Banday/

http://www.researchgate.net/researcher/81029649_P_Bhaskar_Reddy/

http://www.researchgate.net/researcher/39665328_K_A_Suri/

http://www.researchgate.net/researcher/60672477_B_D_Gupta/

http://www.researchgate.net/researcher/39814538_N_K_Satti/

http://www.researchgate.net/researcher/81024624_Basant_P_Wakhloo/

http://www.researchgate.net/researcher/14176149_H_M_Sampath_Kumar/

http://www.researchgate.net/researcher/39783788_G_N_Qazi/

http://www.researchgate.net/journal/1381-1177_Journal_of_Molecular_Catalysis_B_Enzymatic

http://www.researchgate.net/journal/1381-1177_Journal_of_Molecular_Catalysis_B_Enzymatic


http://www.researchgate.net/researcher/2028916399_Debabrata_Bhunia/

http://www.researchgate.net/researcher/2028910311_Yogesh_K_Verma/



http://www.researchgate.net/researcher/39772388_Anamika_Khajuria/

http://www.researchgate.net/researcher/40001484_Amit_Gupta/

http://www.researchgate.net/researcher/2028910095_M_Preethi_Pallavi/

http://www.researchgate.net/researcher/2028944588_S_Surya_Vamshi/

http://www.researchgate.net/researcher/14964119_Gulam_N_Qazi/

http://www.researchgate.net/researcher/2028906861_Halmuthur_M_Sampath_Kumar/

http://www.researchgate.net/journal/1878-1705_International_immunopharmacology


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PP-18

Development of Novel Muramyl Dipeptide Analogues as Vaccine Adjuvants

Sreekanth Miryala, S. Suryavamshi, Halmuthur M. Sampath Kumar*

Vaccine Immunology Lab, NPC Division, Indian Institute of Chemical Technology, Hyderabad, 500007,

India

ABSTRACT

Muramyl dipeptide (N-acetylmuramyl-L-alanyl-D-isoglutamine) is a synthetic immunoreactive

peptide consisting of N-acetyl muramic acid attached to a short amino acid chain of L-Ala-D-

isoGln. It was first identified in bacterial cell wall peptidoglycan as an active component in

Freund’s complete adjuvant. In the cell, MDP is detected by NOD2, a cytoplasmic receptor

belonging to the human innate immune system. In an attempt to increase adjuvant activity and

boost the immune response of MDP, we synthesized different N-alkyl derivatives of muramyl

dipeptide and evaluated them for the biological activity, i.e., OVA specific serum antibody titres;

Th1/Th2 mediated cytokine response. The results have shown that some analogues could induce

immune response significantly.

OHOO

HN

HO

ONH

R

OOH

O

HN

O NH2

OH

O

R = alkyl, aryl, cycloalkyl

References:

1. Hasegawa ASE, Hioki Y, Kiso M, Azuma I. Carbohydrate Res. 1984;129:271–77.

2. Merser C, Sinay P, Adam A. Biochem Biophys Res Commun. 1975;66(4):1316–22.

3. Kotani S, Watanabe Y, Kinoshita F, Shimono T, Morisaki I. Biken J.1975;18(2):105–11.

4. Kufer TA, Kremmer E, Banks DJ, Philpott DJ. Infect Immun. 2006;74(6):3115–24

5. Chen CM, Gong Y, Zhang M, Chen JJ. J Biol Chem. 2004;279(24):25876–82.

6. Chedid LA, Parant MA, Audibert FM, Riveau GJ, Parant FJ, Lederer E, Choay JP,

Lefrancier PL. Infect Immun. 1982;35(2):417–24.


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PP-19

Click Inspired Synthesis of Diverse Morpholine Fused 1,5-Triazoles

Somesh Shasi, Kunj B. Mishra and Vinod K. Tiwari*

Department of Chemistry, Faculty of Science, Banaras Hindu University, Varanasi-5, India

*E-mail:[email protected]

ABSTRACT

Azide-alkyne cycloaddition reaction is the efficient and versatile method for the synthesis of 1,2,3-

triazoles exhibiting variety of biological activities including antibacterial, anti-HIV, antitumor,

antitubercular, antiallergic, and glycosidase inhibition[1]. Apart from triazoles, the morpholine

skeletons are another biologically relevant heterocyclic moiety which has excellent medicinal

property and are component of a number of drugs [2]. Herein, an efficient convenient and two step

synthesis of 1,2,3-triazolo[5,1-c]morpholine in conjugation of [1,4] triazole linked

carbohydrate/Alkyl/Aryl/Heterocycle/steroid will be presented. Various terminal alkynes upon

reaction with epichlorohydrin, NaN3, CuSO4.5H2O, and sodium ascorbate underwent nucleophilic

displacement and Cu (I) catalyzed click reaction to give glycoconjugate azido-hydroxy triazole.

Subsequently their propargylation and intramolecular 1,3-dipolar cycloaddition carried out in

DMF under heating conditions delivered the final products in 80-95% yield.


207

(1) Meldal, C. W.; Tornoe, C.; Meldal, M. J. Org. Chem.2002, 67, 3057.

(2) Audouze, K.; Nielsen, E, O.; Peters, D. J. Med. Chem. 2004, 47, 3089.

PP-20

Room Temperature Synthesis of Phosphonate Ester Functionalized 2-Amino-

3-Cyano-4H-Chromenes via One-Pot Multicomponent Reaction

Goutam Brahmachari*and Sujay Laskar

Laboratory ofNatural Products and Organic Synthesis, Department of Chemistry, Visva-Bharati (a



ABSTRACT

Organophosphorus compounds are well known for their immense biological activities and also

regarded as important substrates in the study of various biochemical processes [1]. Very

particularly, phosphonates and their derivatives have recently drawn keen attention to the

researchers working in diverse fields due to their promising applications as enzyme-inhibitors,

metabolic probes, peptide mimics, antibiotics, and many more [2]. Examples of numerous

bioactive natural products bearing C–P bond(s) are also known in literature [3]. Under this

purview, development of efficient protocols for the synthesis of phosphonates, phosphonic acids

and related compounds via C–P bond formation is warranted and receiving growing interest to the

synthetic organic chemists. On the other hand, 2-amino-4H-chromene scaffolds represent a

“privileged” structural motif well-distributed in naturally occurring compounds with a broad

spectrum of pharmacological efficacies [4]. Such wide range of promising biological activities and

pharmacological properties of both phosphonate derivatives and 2-amino-4H-chromenes have

created a stir in generating new approaches for the synthesis of a variety of phosphonate derivatives

coupled with 2-aminochromenyl rings, and available methods for these derivatives utilizing

multicomponent reactions (MCRs) as a key step are limited till to-date [2].

As a part of our continuing efforts to develop green synthetic methodologies for useful

organic transformations, a facile and efficient protocol for one-pot three-component synthesis of

structurally diverse (2-amino-3-cyano-4H-chromen-4-yl) phosphonic acid diethyl esters from the




208

reaction of salicylaldehydes, malononitrile (or ethyl cyanoacetate) and triethylphosphite using

basic nanocrystalline MgO as catalyst in aqueous ethanolic medium at room temperature has been

developed. Nano-MgO has been prepared using a simple sol-gel approach. The significant features

of this newly developed eco-friendly green protocol include operational simplicity, easy

reusability of the catalyst, room temperature condition, energy-efficiency, clean reaction profiles,

and good yields (Scheme 1). Overall results and experimental details will be presented at the

Conference Meeting.

Scheme 1. Three-component one-pot synthesis of (2-amino-3-cyano-4H-chromen-4-

yl)phosphonic acid diethyl esters

References

[1] Xu Q.; Zhou, Y. B.; Zhao, C. Q.; Yin, S. F.; Han, L. B. Mini-Rev. Med. Chem.2013, 13, 824-

835.

[2] Brahmachari, G.; Laskar, S. Phosphorus Sulfur Silicon Relat. Elem. 2014, 189, 873-888.

[3] Fields, S. C. Tetrahedron1999, 55, 12237-12273.

[4] Laskar, S.; Brahmachari, G. Signpost Open Access J. Org. Biomol. Chem. 2014, 2, 1-50.

PP-21

Facile and Eco-Friendly Synthesis of 3,3-Bis(Indol-3-yl)Indolin-2-ones and

2,2-Bis(Indol-3-yl)acenaphthylen-1(2H)-one Derivatives at Room

Temperature via One-Pot Pseudo-Multicomponent Reaction

Goutam Brahmachari*and Bubun Banerjee

Laboratory of Natural Products and Organic Synthesis, Department of Chemistry, Visva-Bharati (a



ABSTRACT




209

Indoles and their derivatives represent a “privileged” structural motif well-distributed in

naturally occurring compounds with a broad spectrum of significant biological activities. Oxindole

(indolin-2-one) framework is a privileged heterocyclic motif in numerous bioactive natural

products such as arundaphine, donaxaridine, paratunamide, maremycins, and convolutamydine,

and also in a series of pharmaceutically active compounds. In addition, bis(indolyl)indolin-2-ones

are also found to possess significant anti-inflammatory, anti-HIV, and antitumor activities.

Recently, a series of synthetic 3,3-bis(indol-3-yl)indolinoneshas been evaluated to possess potent

spermicidal potential, anticancer, and cytotoxic properties. Interestingly, certain

bis(indolyl)indolin-2-one derivatives have been reported to exhibit strong cytotoxicity against a

series of cancer cell lines but not against the normal cells. Such handful of diverse applications of

3,3-bis(indol-3-yl)indolinoneshas drawn considerable interest to the synthetic chemists, and as a

result of which a good number of methods for their synthesis have been reported so far. Still there

needs to develop a operationally simple and straightforward protocol for the synthesis of 3,3-

bis(indol-3-yl)indolinones as well as 2,2-bis(indol-3-yl)acenaphthylen-1(2H)-one scaffolds,

which would satisfy with the goal of sustainable and ‘green’ chemistry!

Under this purview, we have been motivated to develop a ‘green’ synthetic protocol for the

title compounds as a part of our continuing efforts in developing green synthetic methodologies

for biologically relevant chemical entities. Hence, we have recently developed a simple,

straightforward and highly efficient one-pot synthesis of pharmaceutically-interesting diverse kind

of 3,3-bis(indol-3-yl)indolinones and 2,2-bis(indol-3-yl)acenaphthylen-1(2H)-one scaffolds using

low-cost and environmentally benign commercially available sulfamic acid as a reusable organo-

catalyst via pseudo-multicomponent reaction of indoles and isatins or acenapthaquinone in

aqueous ethanol at room temperature. The salient features of our present pseudo-MCR protocol

are mild reaction conditions, excellent yields, high atom-economy, environmentally benign, easy

isolation of products, no column chromatographic separation, and reusability of reaction media.

Overall results and experimental details will be presented at the Conference Meeting.

Related Literature

[1] Sridhara, S. K.; Saravanana, M.; Ramesh, A. Eur. J. Med. Chem. 2001, 36,615-625.

[2] Brahmachari, G.; Banerjee, B. J. Chem. Res. 2014, 38, 745-750.

[3] Brahmachari, G.; Banerjee, B. ACS Sustainable Chem. Eng. 2014, 2, 2802-2812.

[4] Brahmachari, G.; Banerjee, B. ACS Sustainable Chem. Eng. 2014, 2, 411-422.

[5] Brahmachari, G. (Editor), Green Synthetic Approaches for Biologically Relevant

Heterocycles, Elsevier Inc., Waltham, MA, USA, 2014, ISBN: 978-0-12-800700-0

[6] Brahmachari, G., Room Temperature Organic Synthesis, Elsevier Inc., Waltham, MA,

USA, 2015; ISBN: 9780128010259

PP-22


210

Dithiocarbamates of ω-substituted (2-naphthyloxy) alkanes: A novel class of

antimicrobial agents.

Sadaf Zaidi,a,c Chandan Kumar,d Mohammed Shariq Iqbal,b Brijesh Pandey,b Nitin Srivastava,c Devdutt

Chaturvedi,a,*



bAmity Institute of Biotechnology, Amity University Uttar Pradesh (AUUP), Lucknow Campus, Lucknow-

226028, U. P.

c Amity School of Applied Sciences, Amity University Uttar Pradesh (AUUP), Lucknow Campus,


dDepartment of Chemistry, S. P. College, S. K. M. University, Dumka-814101, Jharkhand, India.


ABSTRACT

In recent years, dithiocarbamates have received much of our attention due to their wide

utility in the field of pharmaceuticals, agrochemicals, intermediates in organic synthesis,

protection of amino group in peptide chemistry, combinatorial chemistry, and ligand for soft metal

complexation, synthesis of nanoparticles, synthesis of ionic liquids and as useful synthon in

organic chemistry. As a potential versatile synthon, dithiocarbamates have been utilized for the

synthesis of structurally diverse biologically potent compounds like isothiocyanates, thioureas,

cynamide, dithiobenzophene, glycosides, amide and heterocyclic compounds. Furthermore, the

role of the dithiocarbamate linkage has been extensively studied in structurally diverse

natural/semisynthetic molecules against various diseases such as anticancer, antibacterial,

antifungal, antimalarial, antiviral, anti-HIV, antiestrogenic, antiprogestational, antiosteoporosis,

antiinflammatory, antifilarial, antitubercular, antidiabetic, antiobesity, anticonvulsant,

antihelminthes, anti-alzheimer drugs, and CNS and CVS active agents In recent years, researchers

around the globe are emphasizing on antimicrobial activity of natural/semisynthetic/synthetic

dithiocarbamate. In continuation with our research work upon synthesis and bioevaluation of

dithiocarbamates, we have synthesized a novel series of dithiocarbamates ω-substituted (2-

napthaloxy) alkanes I and investigated their antimicrobial activity. Interestingly, majority of them

have shown manifold antimicrobial activity as compared to sample drugs which we will represent

in our presentation.




211

O

S

S

N

prototype IR2

R1

n

References:

(a)Chaturvedi, D.* et al.TetrahedronLett. 2003, 44, 7637-7639; (b) TetrahedronLett.2006, 47,

1307-1309; (c) TetrahedronLett.2007, 48, 149-151; (d) TetrahedronLett.2007, 48, 5043-5045;

(e)Synthesis, 2008, 355-357; (f) TetrahedronLett.2008, 49, 4886-4888; (g) Curr. Org.

Chem.,2011, 15, 1593-1624; (h) Tetrahedron Lett., 2012, 53, 5398-5401; (i) Tetrahedron,2012,68,

15-45; (j) Curr. Org. Chem., 2012, 16, 1609-1635; (k) Synlett.,2012, 23, 2627-2630; (l) Org.

Biomol. Chem., 2012, 10, 9148-9151; (m) Synlett.,2013, 24, 33-36.

PP-23

Role of Flavonoids as Neuroprotector in Cerebral Ischemia

Abdul Basit, Aleza Rizvi, Anuradha Mishra, P Bagga and Mohd. Ahmad

Faculty of Pharmacy, Integral University, Lucknow, India

ABSTRACT

Cerebral Ischemia (stroke) is one of the foremost causes of high morbidity and mortality for both

developed and developing countries. Cerebral ischemia or brain ischemia is a condition that occurs

when there isn’t enough blood flow to the brain to meet metabolic demand. This leads to limited

oxygen supply or cerebral hypoxia and leads to the death of brain tissue, cerebral infarction, brain

is particularly susceptible to the damage due to oxidative stress because neurons are rich in

polyunsaturated fatty acids and levels of endogenous antioxidant enzymes in neuronal tissue are

low.Therefore, oxidative stress may contribute to neuronal cell death due to ischemia and

reperfusion. Several synthetic free radical scavengers have been evaluated in animal models of

cerebral ischemia and reperfusion and have been shown to be protective

Flavonoids are the most potent and versatile biologically active compounds in plant and have been

known as outstanding antioxidant and neuroprotection. Their antioxidant effects were confirmed

to stem from the ability to inhibit lipid peroxidation, chelate redoxactive metals and attenuate other

processes involving reactive oxygen species (ROS).

Flavonoids such as quercetin tilianin, agastachoside, acacetin, apigenin, luteolin, kaempferol,

isorhamnetin, syringaresinol and some anti-oxidants are betacarotene, cannabidiol, pegrogotein

were also reported to protect neurons against injury induced by neurotoxins, suppress neuro-

inflammation and promote memory, learning and cognitive function.


212

Studies are now being focused on to look for flavonoids from different plants that can prevent

transient cerebral ischemia.

Key Words: Stroke, Ischemia, Flavonoids

PP-24

Role of Tellurium Metalloid in Drugs

Sangeeta Bajpai

Department of Chemistry, Amity School of Applied Sciences

Amity University Uttar Pradesh, Lucknow Campus, Lucknow-226028, U. P.

ABSTRACT

Compounds of metalloids viz. Boron, Silicon, Germanium, Arsenic, Antimony, and Tellurium

play a significant role in .drugs. These drugs are used to treat various diseases. Benzoxaboroles

(Boron-based drugs) are used as potential treatments for neglected tropical diseases,

Arsphenamine and Arsenic trioxide Arsenic based drug) has been used to treat syphilis.and acute

promyelocytic leukemia respectively. Pentavalent Antimony compound drugs find use for treating

visceral and cutaneous leishmaniasis. Some drugs containing organosilicon compounds are

effective in vitro multidrug-resistance reverting agents. Tellurium, a rare element, despite of its

relative abundance in the human body has been regarded as a non-essential trace element . Its

chemistry is widely known but its biochemistry is not clearly established to date. Some work based

on its properties is in progress. For example Inorganic tellurane, organotellurides and

diorganoditellurides showantioxidant effects and immunomodulatory effects. Tellurium (IV)

compounds find its application in thiol redox biological activity in the human body. For the

commonly known Parkinson’s disease, ammonium trichloro (dioxoethylene-O, O’-) tellurate

(AS101) isa promising agent. An organotellurane compound, C13H22N+C3H3Cl4OTe-, has been

proved to be toxic against promastigotes and amastigotes. Cadmium telluride nanoparticles are

fluorescent and may be used as quantum dots in imaging and diagnosis. Some unsymmetrical 2-

naphtyl diorganyltellurium dichlorides were most effective organotelluranes with gram-negative

antibacterial effect. The synthesis and X-ray crystal structures of various organotellurium –

dihalides, -dicarboxylates, -di thiocarbamates etc. are reported by our group, but their natural


213

biological functions are not explored. The present work is focused on biological functions of

Organotelluriums.

Keywords: Organotelluriums, Biological activity

PP-25

Anti-Inflammatory and Analgesic Activity of Madhuca Indica Leaf Extracts

Prakash Deep, Amrit Kr. Singh, Suchita Dubey

Amity Institute of Pharmacy, Amity University Uttar Pradesh, Lucknow Campuss.

ABSTRACT

Anti-inflammatory and analgesic activities were evaluated in petroleum ether, alcohol and

aqueous extracts of dried leaves of Madhuca indica (Sapotaceae). The same extracts were

evaluated for preliminary phytochemical investigation. In phytochemical investigation, the

extracts were found to contain alkaloids, carbohydrates, tannins, saponins, phytosterols, proteins

and amino acids. TLC studies of petroleum ether, alcoholic and aqueous extracts was performed.

Petroleum ether 60-80°C extracts showed two spots with Rf values were 0.123 and 0.137.

Alcoholic extracts showed three spots having Rf values 0.115, 0.404 and 0.785. Aqueous extract

showed two spots with Rf values 0.458 and 0.648 respectively. Moisture content, ash value, acid

insoluble ash value and water soluble ash value was found to be (13.70, 0.354 and 5.06)

respectively. 400 and 800mg of extracts of Madhuca indica (PEMI, ALMI and AQMI)

administrated to study analgesic and anti-inflammatory activity. In hot plate method the leaves

extracts of ALMI and AQMI (400 and 800mg) showed increase in latency time as compare to

control (p<0.001) but less than standard. It showed mild analgesic activity but petroleum ether

extract showed no significant antinociceptive activity (p>0.05). In carrageenan induced rat paw

edema, the ALMI and AQMI (400 and 800mg) extract showed significant paw edema inhibition

(p<0.001). These results proved that the anti-inflammatory and analgesic effect of the extract as

claimed in folklore medicine which may be mediated by inhibition of prostaglandin synthesis as

well as central inhibitory mechanism.

PP-26

A Review on Tregitopes Prediction and Its Application as Active

Pharmaceutical Ingredients

Prateek Shukla and Satarudra Prakash Singh*


214

Amity Institute of Biotechnology, Amity University Uttar Pradesh (Lucknow Campus), Malhaur, Gomti

Nagar Extension, Lucknow- 226028

*Corresponding author email: [email protected]

ABSTRACT

Tregitopes (regulatory T-cell epitopes) are MHC class II-restricted promiscuous epitopes and are

located in the Fc and the Fab regions of IgG [1]. They are conserved across IgG isotypes and

mammalian species. In contrast, Tregitopes are not found in other antibody isotypes (IgE, IgA,

and IgM). When it is added in vitro and in vivo, for human PBMC and in animal models, these

Tregitopes activated regulatory T cells (Tregs), increased expression of the transcription factor

FoxP3, and induced IL-10 expression in CD4+ T cells. Furthermore, some studies also

demonstrated the feasibility of modulating CD8+ T-cell reactivity to an antigen using Tregitopes

[2]. The discovery of Tregitopes in IgG and other autologous proteins may contribute to improved

understanding of the mechanism of action of intravenous immunoglobulin G (IVIG), and lead to

the use of these powerful immunomodulators to improve transplantation success and suppress

autoimmune disease [3]. Hence, Tregitope may have applications in any of the autoimmune

diseases that are currently treated almost exclusively with intravenous immunoglobulin G (IVIG),

such as Multiple sclerosis, and allergy where Tregitopes may provide a means of inducing antigen-

specific tolerance.

Key words: Tregitopes, MHC, Immunomodulator, T- cell, Antigen

References:

1. De Groot AS, Moise L, McMurry JA, Wambre E, Van Overtvelt L, Moingeon P, Scott

DW, Martin W. Activation of natural regulatory T cells by IgG Fc-derived peptide

"Tregitopes". Blood. 2008; 112(8):3303-11.

2. De Groot AS, Cousens L, Mingozzi F3, Martin W.Tregitope peptides: the active

pharmaceutical ingredient of IVIG? Clin Dev Immunol. 2013; e493138.

3. Cousens L, Najafian N, Martin WD, De Groot AS. Tregitope: Immunomodulation

powerhouse. Hum Immunol. 2014; 75(12):1139-46.

PP-27

Deimmunization of Biotherapeutics: Current Status and Future Prospects

Bishal Verma and Satarudra Prakash Singh*


215

Amity Institute of Biotechnology, Amity University Uttar Pradesh (Lucknow Campus), Malhaur, Gomti

Nagar Extension, Lucknow- 226028

*Corresponding author email: [email protected]

ABSTRACT

Proteins represent the fastest-growing class of pharmaceuticals for a diverse range of clinical

applications. However, the immune system reacts to T-cell epitope sequences in non-human

proteins, leading to neutralization and elimination by the immune system. One may eliminate

immunogenic peptide fragments by mutating the cognate amino acid sequences, but deimmunizing

mutations are constrained by the need for a folded, stable, and functional protein structure. These

two concerns may be competing, as the mutations that are best at reducing immunogenicity often

involve amino acids that are substantially different physicochemically [1]. Computational protein

design has the potential to create a novel class of therapeutics with tunable biophysical

properties. The present study, review the computational protein design methods for reducing

immunogenicity by eliminating known and predicted T-cell epitopes and maximizing the content

of human peptide sequences without disrupting protein structure and function. For example,

EpiSweep, simultaneously optimizes both concerns. There are various algorithms which identifies

sets of mutations making such Pareto optimal trade-offs between structure and immunogenicity,

embodied by a molecular mechanics energy function and a T-cell epitope predictor, respectively

[2, 3]. They integrate structure-based protein design, sequence-based protein deimmunization, and

algorithms for finding the Pareto frontier of a design space [4]. Hence, computational tool may

prove useful in expanding the repertoire of next-generation biotherapeutics.

Key words: epitope, prediction, biotherapeutics, mutation, protein

References:

1. King C, Garza EN, Mazor R, Linehan JL, Pastan I, Pepper M, Baker D. Removing T-cell

epitopes with computational protein design. Proc Natl Acad Sci U S A. 2014;

111(23):8577-82.

2. Parker AS, Choi Y, Griswold KE, Bailey-Kellogg C. Structure-guided deimmunization of

therapeutic proteins. J Comput Biol. 2013; 20(2):152-65.

3. Salvat RS, Parker AS, Choi Y, Bailey-Kellogg C, Griswold KE. Mapping the pareto

optimal design space for a functionally deimmunized biotherapeutic candidate. PLoS

Comput Biol. 2015; 11(1):e1003988.

4. Salvat RS, Parker AS, Guilliams A, Choi Y, Bailey-Kellogg C, Griswold KE.

Computationally driven deletion of broadly distributed T cell epitopes in a biotherapeutic

candidate. Cell Mol Life Sci. 2014; 71(24):4869-80.

PP-28


216

Influence of standardized aqueous fruit extracts of Luffa Cylindrica on

oxidative stress markers and limpidity of isolated adult goat lenses on hydrogen

peroxide induced cataract: A possible alternative for senile cataract

Suchita Dubey1*, Sudipta Saha2, Shubhini A Saraf2

1Amity University Uttar Pradesh, Lucknow Campus, 226010, Uttar Pradesh, INDIA

2Department of Pharmaceutical Sciences, School of Bioscience and Biotechnology

Babasaheb Bhimrao Ambedkar University (A Central University)

Lucknow- 200265, Uttar Pradesh, INDIA

ABSTRACT

The ability ofLuffa cylindrica Roemfruit extract [LCE] to modulate biochemical parameters was

investigated by in vitro studies for its role in hydrogen peroxide induced cataract on isolated goat

lenses incubated in aqueous humour for 72 hours at 37°C. Test group contained 5, 10, 15, 20, 25

and 30 µg/ml of LCE along with 1 ml of H2O2 (0.5 mM) as negative control. Positive control used

was catalin. After incubation, lenses were examined for morphological variation and biochemical

parameters such as superoxide dismutase (SOD), reduced glutathione (GSH), total protein content

(TPC) and malondialdehyde (MDA). SOD, GSH and TPC level were found to increase

proportionally with the concentration of LCE. However, MDA level were found to be inversely

proportional to the concentration of LCE. Cataract stages were graded at regular intervals.

Morphological examination suggested that LCE (25 µg/ml) maintained vision upto 44 hours than

positive control which could maintain vision for 33 hours.No lens in test group developed dense

nuclear opacity after 24 hours as opposed to 80% in negative control. The results suggest that LCE

can delay the onset and/or prevent the progression of cataract which can be attributed to presence

of adequate phenolics, flavonoids and vitamin A.

PP-29

A facile deoxygenation protocol of benzylic alcohols using bis (benzotriazole)

methanethione as a vital synthetic auxiliary

Anoop S. Singh, Dhananjay Kumar, and Vinod K. Tiwari*

Department of Chemistry, Faculty of Science, Banaras Hindu University, Varanasi 221 005

E-mail:[email protected]

ABSTRACT



217

Deoxygenation plays an important role in numerous synthetic transformations. A most well-

known reaction for the deoxygenation is Barton–McCombie deoxygenation,1 In the classical

Barton–McCombie deoxygenation, readily desulfurization in fairly mild reaction condition of

thiocarbonyl moiety is most common problem, but Deoxygenation via bis(benzotriazole)

methanethione give number of advantages: firstly their preparation from the readily available

benzotriazole is an easy process, long term stability of benzotriazole derived thiocarbamate

intermediate and moreover, these compounds should incorporate a relatively more weaker

benzylic C-O bond rather than benzotriazolyl N-N bond beta (β) to the thiocarbonyl moiety, which

would likely to be cleaved similar to Barton–McCombie deoxyzation. Additionally, the mentioned

radical deoxygenation rather than conventional heating can also be carried out under microwave

efficiently.

So we introduced a facile two-step deoxygenation protocol of benzylic alcohols using

bis(benzotriazole)methanethione. The benzotriazole derivativebenzyloxy-thioacyl benzotriazoles

(ROCSBt) on reaction with silanes or Bu3SnH under microwave or conventional heating undergo

free radical β-scission ofC-O bond to afford deoxy product. The methodology have a wide scope

as it deoxygenate selectively the benzylic alcohols and offers the use of nontoxic (TMS)3SiH

reagent as an acceptable alternate to Bu3SnH.

References

1 D. H. R. Barton, S. W. McCombie, J. Chem. Soc. Perkin Trans. 1 1975, 16, 1574–1585.

2 (a) D. Kumar, A. Mishra, B. B. Mishra, S. Bhattacharya, V. K. Tiwari, J. Org. Chem. 2013, 78,

899–909; (b) D. Kumar, B. B. Mishra, V. K. Tiwari, J. Org. Chem. 2014, 79, 251-266.

PP-30

Role of Computer Aided Drug Design in Drug Development

Zeeshan Fatima

Amity Institute of Pharmacy, AUUP, Lucknow Campus

ABSTRACT


218

The development of new drugs with potential therapeutic applications is one of the most complex

and challenging process in the pharmaceutical industry. Millions of dollars and man-hours are

devoted to the discovery of new therapeutically agents yet the outcome is very poor as there is

only one compound that becomes drug after long years of hit and trial.

The recent advances in molecular biology and computer technology have led to the computer aided

drug design (CADD) which includes both molecular modeling and quantitative structure activity

relationships. This has accelerated the development at the drug discovery phase in terms of

reducing time and money.

By using computational methods and the 3D structural information of the protein target, we are

now able to identify the detailed underlying molecular and atomic interactions involved in ligand:

protein interactions and thus interpret experimental results in detail. Computer-aided drug

discovery has recently had important successes: new ligands have been predicted along with their

receptor-bound structures and in several cases the achieved hit rates (ligands discovered per

molecules tested) have been significantly greater than with experimental high-throughput

screening.

Strategies for CADD vary depending on the extent of structural and other information available

regarding the target (enzyme/receptor) and the ligands. “Direct” and “indirect” design are the two

major modeling strategies currently used in the drug design process .In the indirect approach the

design is based on comparative analysis of the structural features of known active and inactive

compounds. In the direct design the three-dimensional features of the target (enzyme/receptor) are

directly considered. By using these methodologies we can save out time and money and can

produce new effective drugs for the existing disease.

PP-31

Pharmacological screening of Anti-ulcer Activity of saraca indica in

Experimental Animals

Azmi Lubna, Verma Pritt, Paswan S K , Shukla Ila, Gupta S S, Rao Ch V

Pharmacognosy and Ethnopharmacology Division, CSIR- National Botanical Research Institute,

(Council of Scientific and Industrial Research) Rana Pratap Marg, Post Box No. 436, Lucknow-226001,

Uttar Pradesh, India. Email: [email protected]



219

ABSTRACT

The anti‐ulcer activity ofSaraca indica(caesalpinaceae) has been carried out in albino rats.

First of all study on small group of animals was conducted to know the approximate ulcer

protective activity of various solvents extracts of the plant. Finally, the methanolic extract was

selected out and taken for final study. Anti‐ulcer activity of methanolic extract of the herb was

studied in rats, in which gastric ulcers were induced by oral administration of indomethacin (20

mg/kg) followed by pylorus ligation method. The extract was administered in the dose of 100 and

200 mg/kg intraperitonially to the test group of animals for 3 consecutive days and on fourth day

pylorus part of their stomach was ligated. After four hours of ligation, the rats were subjected for

ulcer index and gastric acid evaluation. The reduction of ulcer index as well as gastric acid output

in extract treated animals was found to be statistically significant with respect to control animals.

The extract exhibited ulcer protection activity in dose dependent manner. Misoprostol was used as

standard drug for ulcer protection.

Keywords: Saraca indica, ulcer index, gastric output, misoprostol.

PP-32

Hepatoprotective Property and DNA Protection Activity of Keramua as

Natural Product

Upma Singh, Pankaj Singh and Mamta Shukla

Nutraceutical laboratory, Department of Biochemistry

Dr RML Avadh University, Faizabad- 224001

CSIR-Indian Institute of Toxicology Research, M.G. Marg, Lucknow-226 001

ABSTRACT

Natural products remain a prolific source for the discovery of new drugs and drug leads from

vedic period. Drug induced hepatotoxicity is still a significant unresolved clinical problem as liver

is the most common site of damage.

Objective: The present study was carried out to evaluateIpomoea aquatica as new source of

natural bioactive molecules having antioxidant potential.

Methodology: In present study, total Phenolic content, free radical scavenging activity by DPPH,

SOD, LPO and FTC method, reducing power, calf thymus DNA damage protection activity and

hepato-protective role of hydroethanolic extract ofIpomoea aquaticaleaf extract on paracetamol

induced cytotoxicity in rat liverhave been monitored.


220

Result: Ipomoea aquaticaforskleafhad the highest TPC and maximum percentage inhibition for

FRSA, SARSA, RP, LPO, FTC scavenging activity and protection against Fenton’s reagent

induced damage in calf thymus DNA.Supplementation of IALE conferred significant protection

against APAP induced injury to primarily cultured rat hepatocytes.

Conclusion: Results showed that Ipomoea aquaticaforskis a rich source of many biomolecules

having antioxidant activities and showed potential utility of mature plant for use in herbal drug

system or as nutritional supplement.

Key words: Total phenolic content, antioxidant, Paracetamol, herbal drug.

PP-33

Phytochemical Screening of Launaea Procumbens for their Biological Activity

Preeti Rawat, Anil kumar, S.K.Tewari and Mahesh Pal*

*Phytochemistry Division, CSIR-National Botanical Research Institute Lucknow -226001, U.P., India.

E- mail : [email protected]

ABSTRACT

Introduction : L.procumbens genus, Launaea belongs to family of Asteraceae. It consists about

40 species growing in dry saline and sandy habitats. It is used in wound healing, sound health,

longevity and food supplement in ayurvedic preparations. Traditionally, it has been also used in

the treatment of rheumatism, painful urination, liver dysfunctions, and reproductive disorders (1-3).

Aim : Phytochemical screening of the methanolic extract and fractions ofL.procumbens revealed

the presence of alkaloids, phenols, tannins, flavonoids, steroids, glycosides and triterpenes. Plant

also indicates the presence of fatty acids in the extract which are beneficial for health.

Methodology :Dried leaves and roots of the plant were milled into powder and then extracted with

methanol in an extractor. The extract was evaporated in a rotatory evaporator and dried by vacuum

pump. The methanolic extract was suspended on water and extracted successively with hexane,

ethyl acetate, chloroform, and butanol fractions, respectively. Different reagents were used for

screening of phytochemicals.



221

Result and Discussion: Dietary fatty acids are a major source of energy. Twenty two fatty acids

in roots and eighteen in leaves were identified. Considerable amount of phenolics and flavonoid

contents were found in methanolic extract which have antioxidant property. Bioactive fractions of

plant having free radical scavenging and antioxidant are used in many diseases.

Key words: Fatty acid, Launaea procumbens. Antioxidant.

References: (1) Wazir SM, Saimas , Dasti AA and Subhan S . Ethanobotnical importance of salt

range speciesof district karak .Pakistan .J .Plant Sci.(2007) 13:29-31.

(2) Parekh J and Chanda S. Screening of aqueous and alcoholic extracts of some Indian

medicinal plants for antibacterial activity. Indian .J.Pharm.Sci.(2006) 68:835-838.

(3) Ahmad M, Khan MA,Manzoor S, Zafar M and Sultana S .Check list of medicinal flora of

tehsil Isakhel . District Mianwali Pakistan .Ethnobotanical Leaflets.(2006)10:41-48.

PP-34

Evaluation of the Gelling Behaviour of Different Natural Gums for its

Formulation Prospects

Rachit Mohan, Shobha Singh, Geetendra Kumar & Manjoosha Srivastava

Phytochemistry Division

CSIR-National Botanical Research Institute, Lucknow-226001

Email Id: [email protected]

ABSTRACT

With the availability of the natural polymers, greater success has been achieved in developing the

most promising therapeutic systems, which provides an effective therapy to the patients for

prolonged periods. The delivery systems employing hydro-gels for controlled release can be

categorized into reservoir and matrix devices. The release of drug is dependent on the diffusion of

water into the matrix followed by the dissolution of the drug and finally the diffusion of the

dissolved drug from the matrix. Generally, inert polymer matrices are considered to prepare this

kind of delivery systems of late bio-degradable polymers have also been used to design such

systems. The properties of the formulations may be tailored by substitution of gums to explore its

potentiality as additives and gelling agents in different formulations such as hydro-gels and



222

microcapsules. Polymers obtained from different natural sources had been utilized here as gelling

agents to take a closer leap towards their applications in formulation development and their

comparative study with the synthetic polymers was also conducted. We have characterized and

evaluated the potentiality of the natural polymers to be used in different formulation and compared

it with the more commercially acceptable polymers. The studies conducted may be utilized in the

preparation and development of various type of gel formulation of varying ranges of viscosity,

stability and other characteristics.

Keywords: Gum, Hydro-gels, Bio-degradable, Formulation

PP-35

The Anti-Aging Molecule: Vitamin-E

Parul Tripathi*and Aditi Singh

Amity Institute of Biotechnology, Amity University, Lucknow Campus.

ABSTRACT

- - - - -,

-tocotrienols. Tocotrienols differ from the corresponding tocopherols only in the position

of their aliphatic tail. Tocopherols have a phytyl side chain attached to their chromanol nucleus,

whereas the tail of tocotrienols is unsaturated and forms an isoprenoid chain. Vitamin E is present

in cellular membranes where it effectively inhibits the peroxidation of lipids. Tocopherols and

tocotrienols possess the capability to scavenge the chain-propagating peroxyl radical. Prior studies

-tocopherol has the highest biologic activity and it is generally accepted to be the most

-tocopherol is a more

-tocopherol. Tocopherols in the food seem to be beneficial

in maintaining cardio-vascular health. In humans, severe vitamin E deficiency leads to

neuromuscular abnormalities characterized by spinocerebellar ataxia and myopathies. The

peripheral neuropathy likely occurs due to free radical damage to the nerves and degradation of

the sensory neurons. Also, Vitamin E deficiency causes anemia, largely in premature infants,

which is a result of free radical damage. Vitamin E is lipid-soluble vitamin comprised of a family

of 8 stereoisomers characterized by a chromanol ring with a phytyl side chain referred to as

tocopherols and tocotrienols. The molecular mechanism of vitamin E which plays a role in a

variety of physiological and biochemical functions is probably mediated either by the antioxidant

function or its membrane stabilizing effect.

Keywords: Vitamin E, tocopherols, tocotrienols, antioxidant, etc.

PP-36


223

Indicator of Foreign Invasion to the Human Body: Histamin

Vipul Verma and Rachana Singh

Amity Institute of Biotechnology, Amity University Uttar Pradesh, Lucknow Campus.

[email protected]

ABSTRACT

Histamine is a chemical compound involved in immune responses. Histamine is involved in

the inflammatory response. As a response to the invading pathogens or any foreign particles,

histamine is produced by basophils and by mast cells found in nearby connective tissues.

Histamine increases the permeability of the capillaries to white blood cells and required molecules,

to allow them to engage pathogens in the infected tissues. Histamin comes into action whenever

there is a tissue injury i.e. any physical or chemical agent that injured tissue, skin or mucosa, during

anallergic reaction i.e. when there is an exposure of an antigen to a previously sensitized (exposed)

subject or due to drugs and other foreign compounds like morphine, dextran, antimalarial drugs,

antibiotic bases, alkaloids, Penicillins, Tetracyclines, etc. Histamin acts in a receptor mediated

response. Generally three histamin receptors are studied in human body, such as, H1 receptors

which mediate effects on smooth muscle leading to vasodilation, increased vascular permeability,

and contraction of nonvascular smooth muscle, H2 receptors which mediate histamine stimulation

of gastric acid secretion and may be involved in cardiac stimulation & H3 receptors which act as

feedback inhibitors in CNS, gastrointestinal tract, lung, heart.Antihistamines work by blocking the

chemical messenger histamine. Antihistamines are effective and generally safe. They lessen the

symptoms of hay fever, hives, and other allergies in a majority of people, though they don’t usually

relieve symptoms entirely. Some of the commonly used anti-histamins are Cetirizine,

Levocetirizine, etc.

Keywords: Histamine, inflammatory response, etc.

PP-37

Biosensors to be a Potential Technique for Medical Applications


http://en.wikipedia.org/wiki/Immune_system

http://en.wikipedia.org/wiki/Inflammatory_response

http://en.wikipedia.org/wiki/Basophil

http://en.wikipedia.org/wiki/Mast_cell

http://en.wikipedia.org/wiki/Inflammatory_response


224

Adrija Chowdhury, Shruti Mishra and Ashok Kumar Mishra*

Opto-Electronics Laboratory, Department of Physics

Amity University Uttar Pradesh, Lucknow Campus, India- 226028

Email: [email protected], [email protected], [email protected]

ABSTRACT

Besides the difficulty being faced in converting the biological phenomenon into detectable

electrical signal, remarkable progress has been witnessed in the field of biosensors capable enough

to overcome this difficulty. These are the class of sensors that make use of analyse to sense the bio

phenomenon and embedded with the transducer to generate electronic signal to be processed and

displayed accordingly. With glucose monitoring in diabetic patients being the most common

application of biosensor in daily life, researches have led us to other applications like detection of

bacterial pathogens or antibodies like parasite in blood, detection of levels of toxic substances,

detection of cardiovascular & congenital diseases, cancer detection, cholesterol measurement,

measurements of metabolites in media other than blood for non-invasive sensing and smart

application like wearable sensors for healthcare monitoring. The present paper discusses the

potential role of biosensor for developing the ubiquitous health care solutions and subsequent

medical applications. The present study encourages researchers to develop a low-cost, disposable

and user friendly bio sensing device applicable for clinical diagnostics, fall-detection, effective

monitoring to be a major driving force for the expansion of biosensor technologies.

PP-38

Biopesticides: Novel substitutes to Chemical pesticides

Saba Hasan, Maitreyi Mishra and Mohammad Israil Ansari

Amity Institute of Biotechnology, Amity University Uttar Pradesh (Lucknow Campus), Gomti Nagar

Extension, Lucknow (UP)

ABSTRACT

Agriculture and forests form an important resource to sustain global economical, environmental

and social system. For this reason, the global challenge is to secure high and quality yields and to

make agricultural produce environmentally compatible. Chemical means of plant protection

occupy the leading place as regards their total volume of application in integrated pest management

and diseases of plants. But pesticides cause toxicity to humans and warm-blooded animals. The



225

harmful environmental implications of the synthetic chemicals have compelled to search for some

alternative methods. This leads to increased development of compounds based on the models of

naturally occurring toxins of biological origin, having various biological activities. Biopesticides

are biochemical pesticides that are naturally occurring substances that control pests by nontoxic

mechanisms. The most commonly used biopesticides are living organisms, which include

biofungicides (Trichoderma), bioherbicides (Phytopthora) and bioinsecticides (Bacillus

thuringiensis). The potential benefits to agriculture and public health programmes through the use

of biopesticides are considerable, as in being inherently less harmful, designed to affect only one

specific pest or, in some cases, a few target organisms, often effective in very small quantities and

decompose quickly, thereby resulting in lower exposures and largely avoiding the pollution

problems. The demand for bio-pesticides is rising steadily in all parts of the world. Therefore, there

is a need to develop biopesticides which are effective, biodegradable and do not leave any harmful

effect on environment.

Key Words: Biopesticides, Biofungicides, IPM, toxic, pathogenic

PP-39

Evaluation of Anthelmintic Activity of Various Extracts of Annona squamosa

Bark.

Sandeep Sachan1*, Angshu Banerjee2, Rahul Shukla3, Ashutosh Mishra1

1. A.N.D. College of Pharmacy, Babhnan, Gonda.

2. Jyoti Vidyapeeth Women’s University Jaypur, Rajesthan, India.

3. Amity Institute of Pharmacy, AUUP, Noida, India.

ABSTRACT

Annona squamosa Linn (Family Annonaceae) is also called as sugar apple. Different species of

Annona are native to the tropical America. Plant ranges from 10 to 20 ft (3-6 m) in height with an

open crown of irregular branches, and somewhat zigzag twigs. It bears deciduous leaves,

alternately arranged on short, hairy petioles, and is lanceolate or oblong, blunt tipped. All parts of

plants were used in folk medicines from ancient time. It contains various chemical constituents,

including alkaloids, flavonoids and phenols. In the present study an attempt was made to evaluate

its anthelmintic activity of various extracts ofAnnona squamosa Bark. It showed moderate to

significant activity when compared to standard.

Keyword: Annona squamosa, Bark, Folk medicines.


226

PP-40

Evaluation of Hepatoprotective Activity of Acacia Nilotica (Bark) on

Paracetamol Induced Hepatotoxicity

Pritt Verma, Shravan Kumar Paswan Lubna Azmi, Ila shukla, Shayam Sunder Gupta, Ch.V.Rao

Pharmacognosy and Ethnopharmacology Division, CSIR- National Botanical Research Institute,

(Council of Scientific and Industrial Research) Rana Pratap Marg, Post Box No. 436, Lucknow-226001,

Uttar Pradesh, India.


ABSTRACT

Objective: Protective Effect of Acacia nilotica (Bark) against Paracetamol induced hepatic

damage an experimental study.

Methods: Rats were divided into five different groups (n=6), the group I served as a control, Group

II received Paracetamol (250mg/kg) in sterile water, group III and IV served as treatment and

received 250,500 mg/kg of 50% ethonolic extract of A. nilotica, and group V served as standard

group and received silymarin (100mg/kg). All the treatments were given for 10-28 days and after

rats were euthanized, blood and liver was collected for biochemical and histopathological studies,

respectively.

Results: The 50% ethanolic bark extract ofA. nilotica(250, 500 mg/kg p. o.) showed the

remarkable hepatoprotective effect against Paracetamol induced hepatic damage, and observed

that it shows no any significant change in a normal posture, behavior and body weight in Wistar

rats. The degree of protection was measured by biochemical and antioxidant parameters such as

serum glutamate oxaloacetate transaminase (SGOT), serum glutamate Pyruvate transaminase

(SGPT), alkaline phosphatase (ALP), total bilirubin, and the histopathological profile of liver also

indicated the hepatoprotective nature of this drug.

Conclusion: The bark extracts of A. niloticahas showed dose dependent activity, among which at

the dose level of 250 & 500 mg/kg. The further investigations, the bark extract ofAcacia nilotica

identify the active constituents responsible for hepatoprotection.

Keywords: A. nilotica, Antioxidant, Paracetamol, Silymarin.



227

PP-41

Performance Enhancing Traditional Medicines in Sports

Ila Shukla, Shravan Kumar Paswan, Lubna Azmi, Pritt verma, Chandana Venkateswara Rao

Pharmacognosy and Ethnopharmacology Division, National Botanical Research Institute, Rana Pratap

Marg, Lucknow 226001, Uttar Pradesh, India


ABSTRACT

Aim of the reviewing was to examine the use of "Traditional medicines" in sports. Performance

enhancing drugs are the major threat to integrity of sports. Sports always says that "essential thing

is not conquering but fighting well". While in reality there is a huge pressure on athletes as well as

on their coaches. They have to win the competition and for that they resort to many unfair means

to win the competition. This gives rise to misuse of medicines and other traditional drugs. Many

methods have developed to detect the cases of doping, but every time newer cases came in to light.

Many athletes use traditional medicines to hide their act of doping. In this review we have surveyed

about the use of such traditional medicines being used in doping. At some places even nutritional

supplements are also classified as performance enhancing drugs.

Key words: tetrahydrogestrinone, selective androgen receptor modulators, xenoandrogens.

PP-42

Production of a Novel Thermoplastic from Pseudomonas Aeruginosamtcc 7925:

A Boom for Pharmaceutical Industry

Akhilesh Kumar Singh1,*, Nirupama Mallick2 and Aayushi Pandey1

1Amity Institute of Biotechnology, Amity University Uttar Pradesh Lucknow Campus, Uttar Pradesh,

India 2Agricultural and Food Engineering Department, Indian Institute of Technology Kharagpur,

West Bengal, India

E-mail: [email protected]/ [email protected]


228

Tel: +91-5222-399593, Fax: +91-5222-721934

ABSTRACT

An eye-catching bacterium strain, Pseudomonas aeruginosa MTCC 7925emerging as bioengineer

for the production of a novel short-chain-length-long-chain-length polyhydroxyalkanoate (SCL-

LCL-PHA) thermoplastic co-polymer composed of 3-hydroxybutyric acid, 3-hydroxyvaleric acid,

3-hydroxyhexadecanoic acid and 3-hydroxyoctadecanoic acid monomers. In the present study, a

five-level-four-factor central composite rotary design (CCRD) was applied to find out the

interactive eff ects of four variables viz. ethanol, glucose, ammonium nitrate (NH4NO3) and

potassium dihydrogen phosphate (KH2PO4) on SCL-LCL-PHA thermoplastic co-polymer yield in

P. aeruginosa MTCC 7925.Applying response surface methodology (RSM), a second order

polynomial equation was obtained by multiple regression analysis. All the four variables had

significant impact on the co-polymer yield as revealed by statistical analysis of the results. The

model predicted a maximum yield of 81.1% of dry cell weight (dcw) on setting the concentrations

of ethanol, glucose, KH2PO4 and NH4NO3 at 1.5% (v/v), 1.10% (w/v), 2.79 and 1.86 g l-1,

respectively. The predicted value was verified by validation experiments. A yield of 77.6% (dcw)

was achieved as compared to 68.7% co-polymer yield under traditional ‘one-factor-at-a-time’

technique. This novel thermoplastic co-polymer displayed material properties comparable to

conventional plastics, hence open up new potentials for various applications, such as in the field

of pharmaceutical (retarded drug release and drug carrier), medical (absorbable sutures, surgical

pins, staples, bone plates, film around bone fracture), hygiene products etc.

Keywords: CCRD, PHA, Pseudomonas aeruginosa MTCC 7925, RSM, SCL-LCL-PHA

thermoplastic co-polymer.

Focus area: Pharmaceutical/medicinal chemistry of synthetic/semi synthetic/natural products in

drug discovery research

PP-43

An efficient and novel approach for the syntheses of S-alkyl thiocarbamates

from their corresponding alcohols employing TPP.Br2

Sadaf Zaidi,a,c Neha Singh,e Amit K. Chaturvedi,bNitin Srivastava,d Devdutt Chaturvedi,a,*





229

cDepartment of Chemistry, Amity School of Science and Technology, Amity University Uttar Pradesh



ABSTRACT

S-Alkyl thiocarbamates (S-alkylthiourethanes) constitute an important and versatile class of

compounds for a variety of industrial, synthetic, medicinal applications, pharmaceuticals,

agrochemicals, intermediates in organic synthesis, for the protection of amino group in peptide

chemistry, as linkers in combinatorial chemistry and commercial herbicides. These uses require

their preparation by convenient and safe methodology. Classical synthesis of S-alkyl

thiocarbamates involves phosgene, its derivativesand carbon monoxide. But most of these methods

suffer from the limitations such as long reaction times, use of expensive strongly basic reagents,

tedious work-up and low yields. Consequently, there is continuous interest in developing new and

convenient methods for the synthesis of S-alkyl thiocarbamates using mild reaction conditions.

Our group has been engaged from past several years for the development of new methodologies

for the preparation of carbamates, dithiocarbamates, S-alkylthiocarbamates and related

compounds using cheap, abundantly available, and safe reagents like CO2 and CS2 respectively.

In our ongoing research work on Triphenylphosphinedibromide (TPP.Br2) we found that TPP.Br2

is the best catalyst for the synthesis of S-alkylthiocarbamates, employing a variety of reagents. In

the present paper, we report herein a new and efficient one-pot method for the synthesis ofS-

alkylthiocarbamates 1 through the reaction of corresponding alcohol, amine and CS2 employing

catalytic amount of TPP.Br2 at room temperature (Scheme 1). To the best of our knowledge, this

is the first report for the efficient and mild synthesis of S-alkylthiocarbamates employing TPP.Br2,

afforded good to excellent yields (80-98%).

R1 OH

R2

R3

+ HN

R5

R4 Dry DMSO, TPP.Br2, CS2 R1 O

R2

R3

S

N

R5

R4

1

Scheme 1

RT , 1-2 hr., 80-98%

References:

(a) D. Chaturvedi,* et al, Tetrahedron Lett.2003, 44, 7637. (c) Tetrahedron Lett.2006, 47, 1307.

(d) Tetrahedron Lett. 2007, 48, 149. (e)(f)Tetrahedron Lett. 2007, 48, 5043.; (g) Synthesis 2008,

355-357; (h) Tetrahedron Lett.2008, 49, 4886-4888; (i) )Tetrahedron Lett.,2012,53, 5398-5401;(j)

Tetrahedron, 2012, 68,15-45; (k) Synlett.,2012, 23, 2627-2630; (l) Org. Biomol. Chem.,2012,10,

9148-9151; (m) Synlett.,2013,




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PP-44

In-Vitro Antioxidant Activity & Elemental Analysis of Bauhinia.Purpureal.

For its Potential use in Nutraceuticals

Abhishek Gupta, AKS Rawat

Pharmacognosy & Ethnopharmacology Division,

CSIR- National Botanical Research Institute, Lucknow, India-226001

ABSTRACT

The aim of present study was to assess the pharmacognostical, antioxidant and nutritional activity

in ethanolic crude extracts of B. purpurea. All the preliminary pharmacognostical parameters were

determined using standard methods. The total antioxidant activity was assayed by total phenol

content, total flavonoid content, DPPH free radical scavenging assay methods which showed good

antioxidant activity. Elemental Analysis was assessed using ICPMS. Zinc was found to be present

in fair amount as compared to other micronutrients. Chromatographic study was done by using

HPTLC. For achieving good separation ofphenolic compounds a mobile phase of toluene: ethyl

acetate: formic acid (7:3:1) was used and data revealed the presence ofcaffeic, vanillic, syringic

acid and kaempferol in methanolic fraction of flower buds ofB. purpurea. The quantification of

phenolic compounds and antioxidant activity in B. purpurea have not yet been quantified, thus this

information can be useful for proper standardization of herbal drug containing B. purpurea. The

pharmacognostical parameters reported can be considered as quality standards of B. purpureain

herbal industry. The study concluded that ethanolic extracts ofB. purpureahave good antioxidative

potential and can be used in nutraceuticals.

PP-45

Evaluation of Jatropha Glandulifera Extracts for Anti-Inflammatory Activity

and Wound Healing Potential Dwivedi Jyotsana1, Dwivedi Monika1, Gupta Abhishek1, Paliwal S.K2, Rawat A.K.S1٭

1CSIR-National Botanical Research Institute, Lucknow-226001

2Banasthali Vidyapeeth, Banasthali, Rajasthan.

ABSTRACT


231

Ethnopharmacological relevance: Jatropha glandulifera L. is extensively used in Indian

systems of medicine for its medicinal properties including burns, convulsions, fever and

inflammation. The aim of this study was to evaluate the wound healing potential and anti-

inflammatory activity of J. glandulifera.

Material and methods: Various extracts of J. glandulifera were prepared and screened for their

2, 2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging capacity and antioxidant activity using

the NO inhibition assay and inhibition of erythrocytes haemolysis. These extract were subjected

to antibacterial assay and NO inhibition on macrophages J774. Pure extracts were used for in vivo

wound healing experiment. Identification and quantification ofmarker compounds in extracts

were done after fractionation through Flash chromatography by Camag HPTLC.

Results: The present study has demonstrated that the extracts have properties to render them

capable of promoting accelerated wound healing activity compared with placebo control, which

was evidenced by decrease in period of epithelization, increase in rate of wound contraction. There

was no significant hemolytic activity against rat erythrocytes. The antibacterial activity for gram

positive bacteria was observed in all extracts (hydro alcohol, ethanol with pronounced effect in

50% hydroalcoholic extract ofJ. glandulifera followed by ethanol extract ofJ. glandulifera. The

extracts ofJ.glandulifera (2mg/ kg body weight) were given to individual groups were screened

for its effect on bleeding time (BT), clotting time (CT), prothrombin time (PT), platelet count and

platelet adhesion in albino rats after 1-day, 7-day , 14 day and 21-day treatment.The J.

glandulifera showed period of epithelisation of 21day while comparison to this the control had

the wound areamm2 (% of wound contraction) 175 ± 2.86 (67.71) on 21st day. The HPTLC

profiling indicate the reasonable content of all three ursolic acid, lupeol and beta sitosterol markers

in blood coagulation profile of the plant.

Conclusion: Thus results shown by J. glandulifera fractions explain that the sitosterol, lupeol and

urosolic acid present in J. glandulifera extract synergize its antioxidant, anti- inflammatory and

wound healing potential. Lupeol, sitosterol, ursolic acid has been already extensively studied for

its inhibitory effects on inflammation under in vitro and in animal models of inflammation and

wound healing potential.

PP-46

Concomitant Administration of Trikatu With Curcumin as Poly Herbal

Phytoformula for Cancer Chemotherapy

Monika Sharmaa, Vikas Sharmab, Gopal Guptab, Ajay Kumar Sigh Rawata*

1Pharmacognosy and Ethnopharmacology Division, CSIR-National Botanical Research Institute,

Lucknow, (U.P), India

2Endocrinology Division, CSIR-Central Drug Research Institute, Lucknow, (U.P), India


232

ABSTRACT

Background: Curcumin, a natural polyphenol extracted from Curcuma longa L., a golden spice

with broad biological outcomes, exploited for Pure Small Cell Carcinoma. The purpose of this

study is to formulate and evaluate the novel phytoformula of curcumin with natural bioenhancers

for hormone independent cancers. Curcumin when combined with a selective concentrations of

well known natural bioenhancers Piper nigrum, Piper longum and Zingiber officinale, collectively

known as trikatu in ayurveda, synergize the anti-tumourogenic effect along with anti-inflammatory

and anti-oxidant activity .

Methodology: Curcumin combinations (P1, N1 and G1) with natural bioenhancers were

formulated and evaluated for the cytotoxicity, ROS (reactive oxygen species)-generation activity

and radical-scavenging activity, apoptosis (Annexin-PI staining), and caspase-3 assays on PC3

cells. The effect on PGP activity was explored by Hoechst assay and ATPase activity assay.

Results: The anti-cancer formulations P1, N1 and G1 exhibited the highest cellular uptake with

ceiling ultra structural changes related to apoptosis in SCNC. The P1, N1 and G1 showed higher

apoptotic activity at lower concentrations than curcumin (P1 IC50 = 4.7µg/ml, G1 IC50 = 5.2 µg/ml

and G1 IC50 = 6.6 µg/ml). The apoptotic activity of these formulations associated with generation

of ROS by the tumor cells as detected by 2,7 dichloroflouresence diacetate (DCFDA) assay. The

cell uptake studies revealed preferential uptake of curcumin increased in the PC3 cells in following

order: G1>P1> N1. The P1, N1 and G1 have PGP inhibitory effect as shown by ATPase activity

assay and Hoechst assay.

Conclusion: Thus, natural bioenhancer effectively synergizes the effect of curcumin for harmone

independent cancers. These prototype curcumin-bioenhancer formulations have the propensity to

integrate new targeted therapy for treatment of this rare and aggressive tumor.

PP-47

Characterization of chemical constitutions of Boenninghausenia albiflora and

their antioxidant activity

Siddharth pragyadeep, Shikher Verma, Sharad Shrivastav, Ajay Kumar Singh Rawat

Pharmacognosy and Ethnopharmacology Division, CSIR-National Botanical Research Institute,

Lucknow, (U.P), India

ABSTRACT


233

The aim of this study was to screen various extracts prepared from aerial part and root

of Boenninghausenia albiflora for their metabolite profiling and in-vitro antioxidant activity. Arial

part and root were subjected to quantitative screening test for various constituents which revealed

the presence of sugar (6.5 and 8.4%), starch (7.0 and 10%), and tannins (37.5 and 36.96 µg tannic

acid equivalent /mg dry extract), respectively. The order of total phenolic content was descended

in following order: hydro-alcoholic extract of aerial part (HEA)-methanolic extract of aerial part

(MEA) - hydro-alcoholic extract of root (HER)m-ethanolic extract of root (MER). HEA showed

an effective scavenging of DPPH radical (IC50, 195.9µg/mL) followed by MEA (IC50 243.8

µg/mL). While IC50 values for HER and MER were recorded by 370µg/mL and 600µg/mL,

respectively. For achieving good separation of phenolic compounds using HPTLC, a mobile phase

of toluene: ethyl acetate: formic acid (5:5:1) was used and data revealed the presence of caffeic

and ferulic acids in roots and aerial part extracts of B. albiflora. The quantification of phenolic

compounds and antioxidant activity in B. albiflora have not yet been reported, thus this

information can be useful for proper standardization of herbal drug containing B. albiflora.

PP-48

In-vitro antioxidant activity on different extracts of Caesalpinia bonducella

seeds

Shikhar Verma, Abhishek Gupta, Arshad Hussain1, M.V Ramana2, A.K.S Rawat



1Department of Pharmacy, Integral University, Lucknow

3 Institute of Pharmacy, Amity University, Lucknow

ABSTRACT

The Caesalpinia bonducella (Caesalpiniaceae) is a wildly grown plant throughout India and is of

immense medicinal importance. In this study the aqueous, hydro-alcoholic and chloroform extracts

of C. bonducella seeds were screened for antioxidant activity using, DPPH free radical scavenging

activity, total phenolic content (TPC) estimation and β-carotene bleaching assay. IC50of aqueous,

hydro-alcoholic and chloroform extracts was found to be 19.16±1.92 µg/ml,

105.66±3.29µg/mland170±4.08µg/ml respectively and that of ascorbic acid is 2.03±0.16µg/ml.

Total Phenolic Content in all the extracts aqueous, hydro-alcoholic and chloroform shows the

presence of TPC 52.16±1.04, 8.10±1.26 and 1.89±0.28 respectively in 100 µg/ml concentration.

In β-Carotene/linoleic acid assay antioxidant activity of aqueous, hydro-alcoholic and chloroform

extract was found to be 31.99±0.50, 26.58±1.00 and 24.96±0.31respectively. Butylated

hydroxyanisole (standard) show the highest Antioxidant activity of46.70±0.43.The


234

pharmacognostical parameters reported can be considered as quality standards of C. bonducella in

herbal industry. The study concluded that extracts of C. bonducella have good antioxidative


Key words: Caesalpinia bonducella, TPC, DPPH, Antioxidant activity

PP-49

Role of Preclinical Drug Screening to Speed Drug Discovery and Development

Processes

Pratik Khanala, Jyotsna Pandeya, Sujeet Guptaa, Bhumika Yogib and Mehnaz kamalc

a. Hygia Institute of Pharmaceutical Education & Research, Lucknow

b. R.B.S.K. Health department M.P.

c. Faculty of Pharmacy ,Integral University, Lucknow


ABSTRACT

Clinical trials are designed to help us find out how to give a new treatment safely and effectively

to people. The sponsor of the clinical trial needs to gather data regarding safety of a new drug in

small-scale clinical studies before it is studied in humans. Prior to testing on humans clinical trials

involving new drugs are subject to rigorous testing in the laboratory (pre-clinical trials). Pre-

clinical studies involve in vitro (test tube) and in vivo (animal) experiments using wide-ranging

doses of the study drug to obtain preliminary efficacy, safety, toxicity and pharmacokinetic

information. Such tests assist pharmaceutical companies to decide whether a drug candidate has

scientific merit for further development as an investigational new drug. Pre-clinical studies can be

used to identify lead compounds likely to possess favorable biopharmaceutic and pharmacokinetic

properties in humans. In addition, they can facilitate transition through the discovery -

development interface and decrease the need for expensive and time-consuming clinical studies.

http://www.answers.com/topic/in-vitro

http://www.answers.com/topic/in-vivo

http://www.answers.com/topic/efficacy

http://www.answers.com/topic/toxicity

http://www.answers.com/topic/pharmacokinetics


235

The limitations of preclinical studies are suitable pharmacological models have not yet been

developed for many common diseases, extrapolation of toxicity data from animals to humans is

not completely reliable and rare adverse effects are unlikely to be detected. In spite of limitations,

pre-clinical studies serve a vital role in the drug discovery and development processes. There is a

need of ongoing true integration between the preclinical, regulatory and clinical teams for further

growth.

PP-50

Combinatorial Chemistry: A tool for drug discovery and lead optimization

Vandana Singh, Manish Kumar Singh, Ruby Tabassum , Neha srivastava and Sujeet Gupta

Hygia Institute of Pharmaceutical Education & Research, Lucknow


ABSTRACT Combinatorial chemistry has emerged over the last few years as an important tool for drug

discovery and lead optimisation. Combinatorial chemistry has evolved from its early focus as a

random strategy for generating molecular diversity into a powerful design technology for

developing and optimizing drug candidates. Combinatorial chemistry is redefining the way

pharmaceuticals and other high performance chemicals and materials are discovered and

developed. It afforded faster, less expensive and more comprehensive exploitation of new drug

targets.While the techniques of this rapidly growing field are used primarily to find new candidate

drugs, combinatorial chemistry is also finding other applications in various fields such as

semiconductors, catalysts, and polymers. This guide for librarians explains the basics of

combinatorial chemistry and elucidates the key information sources needed by combinatorial

chemists. Combinatorial chemistry has emerged over the last few years as an important tool for

drug discovery and lead optimization. In this approach, the molecular diversity and range of

biological properties displayed by secondary metabolites constitutes a challenge to combinatorial

strategies for natural products synthesis and derivatization.

PP-51

Increasing the Efficacy of Diferuloylmethane as Anticancer Agent by

Increasing Solubility through Nanosization.

Mohini Chaurasia, Monika Kulshreshth


236

Amity Institute of Pharmacy, Amity University Uttar Pradesh, Lucknow Campus

ABSTRACT

Curcumin or diferuloylmethane is an anticancer agent. Free curcumin induces cell cycle arrest and

apoptosis in human cancer lines derived from a variety of solid tumors Despite the considerable

promise that curcumin is an efficacious and safe compound for cancer therapy; the single most

reason for the reticence had been the reduced solubility which may lead to low bioavailability

when given orally and formation of drug aggregates resulting embolism when administered

systemically.

In the present work a nanosized drug delivery system using calcium phosphate; A cheap, easily

available and biodegradable inorganic material was prepared in order to enhance solubility of

curcumin. The NPs were prepared by one step supersaturation synthesis using calcium chloride,

Phosphoric acid, sodium hydroxide (maintain basic pH) and Sodium Citrate (for quenching the

reaction). Nanoparticles so prepared were characterised for its size (zeta sizer, Melvern), size

distribution, drug loading capacity, drug release profile in-vitro., and evaluated for enhanced

solubility. The nanoparticles showed narrow size distribution between 130-200nm with PDI 0.270

and were found to be stable with zeta potential -42.3mV. Drug loading was determined by indirect

method using UV detector, and was found to be 113µg/mg (EE-89%). Dissolution studies

performed on the pellet formed with nano-curcumin and curcumin drug showed 27% higher drug

release (in 24hr) from nanocurcumin pellet in comparison to Curcumin drug, leading to conclusion

that solubility of curcumin has been increased by naosization.

PP-52

Formulation and Development of In-Situ Gel for Ophthalmic Drug Delivery

Dipti Srivastava, Navneet Srivastava

Amity Institute of Pharmacy, AUUP, LKO

ABSTRACT

Topical delivery of eye drops into the lower Cul-de-sac is the most common method of drug

treatment for ocular diseases and diagnosis. Eye drops that are conventional ophthalmic delivery

system often result in poor bioavoilability and therapeutic response since the high tear fluid

turnover and dynamics cause rapid precorneal elimination of the drug. One of the approaches to

overcome the above mentioned problem is in situ gelling system for ocular drug delivery which

increases the retention time and also sustains the release of the drug. The object of the present

investigation is to prepare and evaluate in situ gel-forming ophthalmic drug delivery system of

Moxifloxacin hydrochloride using ion gelation technique. Sodium alginate, a novel ophthalmic

gel-forming mucoadhesive polymer, which gets converted to gel in the presence of divalent-


237

cations (calcium ion) present in the lachrymal fluid, was used as the gelling agent. The copolymer

HPMC was used as viscosity enhancer. Benzalconium chloride was further added as a preservative

and Sodium chloride was added to adjust the tonicity of the formulation. All the formulations were

sterilized in an autoclave at 121°C for 15 minutes. The formulations were evaluated for clarity, pH

measurement, gelling capacity, drug content estimation, rheological study, in vitro diffusion study

and antibacterial activity. Batch F3 showed maximum drug release at the end of 4hrs. Batch F3

also shows antibacterial efficacy with E. coli and S. aureusstrains. These results demonstrate that

the developed system is an alternative to conventional ophthalmic drops.

PP-53

Identification of Novel Anticancer 1,4,5-Trisubstituted 1,2,3-triazoles with -

Amino Alcohol Scaffold as Potent Antimalarial Agents.

N. Devendera, sarika gunjanb, Kartikey singha, venkatareddy pasama, Hamidullahc, sanjeev, K. Shuklad,

Renu tripathib, Rituraj konwarc, Arun Kumar Trivedie and Rama P. Tripathi*a,f.

aMedicinal & process chemistry division, bparasitology division, cEndocrinology division, dSAIF division,

ebiochemistry division, fAcademy of Scientific & Innovative research (AcSIR), CSIR- Central drug

research institute, Lucknow-226031, India.

ABSTRACT

Malaria remains one of the world’s major global health threat and plasmodium falciparum is the

dominant causative agent of most sever forms of malaria in humans. Recently, WHO report

signifying that approximately 627,000 deaths were occurred worldwide in 2012 only. Resistance

to current antimalarial drugs is a key problem and despite the presence of many antimalarial drugs

marketed now, there is a burning need for developing new antimalarials with novel mechanism of

action. Many anticancer compounds reported for example nutlin-3, acted as a useful potent

antimalarials1, which is also benefited by the usefulness against multiple diseases. With these facts

towards the development of new antimalarials with different mechanism, we were synthesised a

novel series of anticancer 1,4,5-trisubstituted 1,2,3-triazoles bearing β-amino alcohol scaffold2

(shown below) and evaluated them for antimalarial activity by in vitro and in vivo.


238

Fig: General prototype of our synthesised molecules.

References:

1. Kaushansky, A.; Ye, A. S.; Austin, L. S.; Mikolajczak, A. M.; Vaughan, A. M.; Camargo,

N.; Metzger, P. G.; Douglass, A. N.; MacBeath, G.; Kappe, S. H. I. CellReports. 2013, 3,

630-637.

2. Ajay, A. Gupt, M. P.; Devender, N. Tripathi, R. P. Mol Divers. 2012, 16, 335-350.

PP-54

A Strategy for the Synthesis of Anthraquinone-Based Aryl‑C‑glycosides

Kartikey Singh1, N. Anand1, S. K. Shukla2δ, R. P. Tripathi*1δ

δAcademy of Scientific and Innovative Research, 1Division ofMedicinal & Process Chemistry,

2Sophisticated Analytical Instrumentation Facility, CSIR-Central Drug Research Institute, Sec. 10,

Jankipuram Extn., Sitapur Road, Lucknow-226031, Uttar Pradesh, INDIA.

ABSTRACT

C-aryl glycosides, both of synthetic and natural origins, are significantly important in

medicinal chemistry owing to their stability toward enzymatic and chemical hydrolysis as

compared to their O- and N-glycosides [1]. They are versatile chiral building blocks in

pharmaceutics and have the potential to act as enzyme inhibitors and stable sugar mimics [2]. One


239

class of medicinally important aryl glycosides, active against diabetes, and currently in late phase

development are the SGLT-2 inhibitor [3]. The angucycline group of glycosides with

anthraquinone as aglycone part is endowed with anticancer, antiviral, enzyme inhibitory and

platelet aggregation inhibition activities [4]. Therefore anthraquinone based C-aryl glycosides

synthesis has attracted considerable interest.

In the work presented here, we provide an efficient and simple strategy for the synthesis of

a diverse range of anthraquinone based C-aryl glycosides. Strategy involves the sequential Diels

Alder reaction and oxidative aromatization with the performed glycosyl diene and dienophile. The

synthesis of glycosyl dienes from simple sugars was achieved by tandem one pot substitution and

elimination reaction.

Reference

1. D. E. Levy et al., The Chemistry of C-Glycosides; Elsevier Science, Ltd.: Amsterdam,

1995; p 4.

2. (a) M. D. Lewis et al., J. Am. Chem. Soc.104, 4976,1982. (b) K. Horika et al., Synlett, 43,

1994.

3. E. C. Chao et al.,Nat. Rev. Drug Discovery, 9, 551, 2010.

4. J. Rohr et al.,Nat. Prod. Rep.9, 103, 1992. (b) M. K. Kharel et al.,Nat. Prod. Rep. 29,

264, 2012.

PP-55

In Vitro Antioxidant Activity on Different Extracts of Caesalpinia Bonducella Seeds

Shikhar Verma, Siddhartha Pragyadeep, Arshad Hussain1, M.V Ramana2, A.K.S Rawat



1Department of Pharmacy, Integral University, Lucknow

4 Institute of Pharmacy, Amity University, Lucknow

ABSTRACT


240

The Caesalpinia bonducella (Caesalpiniaceae) is a wildly grown plant throughout India and is of

immense medicinal importance. In this study the aqueous, hydro-alcoholic and chloroform extracts

of C. bonducella seeds were screened for antioxidant activity using, DPPH free radical scavenging

activity, total phenolic content (TPC) estimation and β-Carotene bleeching assay. IC50of aqueous,

hydro-alcoholic and chloroform extracts was found to be 19.16±1.92 µg/ml,

105.66±3.29µg/mland170±4.08µg/ml respectively and that of ascorbic acid is 2.03±0.16µg/ml.

Total Phenolic Content in all the extracts aqueous, hydro-alcoholicand chloroform shows the

presence of TPC 52.16±1.04, 8.10±1.26 and 1.89±0.28 respectively in 100 µg/ml concentration.

In β-Carotene/linoleic acid assay antioxidant activity of aqueous, hydro-alcoholic and chloroform

extractwas found to be 31.99±0.50, 26.58±1.00 and 24.96±0.31respectively.

Butylatedhydroxyanisole(standard) show the highest Antioxidant activity of46.70±0.43.The

pharmacognostical parameters reported can be considered as quality standards of C. bonducellain

herbal industry. The study concluded that extracts of C. bonducella have good antioxidative


Key words: Caesalpinia bonducella, TPC, DPPH, Antioxidant activity

PP-56

Evaluation of In-Vitro Antioxidant Activity in Four Nephrolepis Species

Shweta Singh, Yogesh Joshi1, P B Khare, A.K.S Rawat



1Department of Botany, S.S.J. Campus, Almora, Kumaun University, Nainital, Uttarakhand

ABSTRACT

The aim of this study was to evaluate in-vitro antioxidant potential of ferns (pteridophytes) which

are lesser explored as compare to angiosperm. In this study, four Nephrolepis species belonging

to family Polypodiaceae were selected viz. N. biserrata (NB), N. cordifolia (NC), N. exaltata (NE)

and N. tuberosa (NT). In performed study alcoholic extracts ofNephrolepis species were screened

for antioxidant activity using DPPH free radical scavenging activity and total antioxidant capacity

(TAC).All the methanolic extracts ofNephrolepis species showed significant DPPH scavenging

ability in decreasing order of scavenging ability and their IC50 values were NT (568.18 mg mL-

1)>NC (609.76 mg mL-1) >NB (892.86 mg mL-1) >NE (961.54 mg mL-1). The total antioxidant

capacity of the extracts (10 mg mL-1) were measured spectrophotometrically at 695 nm based on

the formation of the phosphomolybdenum complex was found to be in NT (321.56) >NC (284.12)


241

>NB (212.16) >NE (152.34) nM of Ascorbic acid per gram. However, high radical scavenging

activity was observed maximum in the N. tuberosa in comparison to other three species for both

DPPH free radical scavenging and total antioxidant capacity assay.

Keywords: Antioxidant, DPPH, Nephrolepis, TAC

PP-57

Assignment and 3D Structure Determination of Ubiquitin from NMR Data

Ms. Tahmeena Khan, Saman Raza

Department of Chemistry, Isabella Thoburn College, Lucknow, India

ABSTRACT

Proteins are the basis of life as they are present in every cell of living beings. They can also

catalyze bio-chemical reactions; can also perform several complex functions like transport of

materials in cells across biological membranes. High resolution NMR spectrum of a protein

contains information on its secondary and tertiary structure. Manual sequential assignment of1H, 13C and 15N spins is tedious and time consuming and therefore there is a need of improved

hardware, automation of analysis and new sources of data such as residual dipolar couplings. The

Aim of the present study was to look for different NMR data processing and assignment softwares

for structure elucidation of protein Ubiquitin, a highly ubiquitous protein having seventy six

Amino acids. Structure determination (3D) of Ubiquitin data of several 3D triple- resonance

experiments were provided in the form of FIDs. A whole lot of programmes have been developed

to perform various steps of structure analysis. In this study NMRPipe was used for the processing

of different spectra where as CCPNmr Analysis was used for sequential assignment of the protein

chain and TALOS (Torsion Angle LikelihoodObtained from Shift and Sequence Similarity) was

used for automated structure calculation. On the basis of analysis done in CCPNmr 5 kinds of

chemical shifts i.e. HN, CA, CB, N & CO were identified and put in TALOS. On the basis of these

chemical shifts TALOS calculated the phi/psi angles of various residues and matched them with

its data base structure and listed the statistics of the ten best data base matches and the best matched

structure was that of Ubiquitin. On the basis of all these parameters the protein was assigned a 3D

structure.

PP-58

Synthesis and characterization of some Schiff base analogs of novel piperidino

tiophenes

Sajal Srivastava1, Barnali Das2


242

1. Amity Institute of Pharmacy, Amity University, Lucknow Campus

2. Berhampur University, Ganjam, Berhampur, Odisha

E. Mail: [email protected], [email protected]

ABSTRACT

It is proved from the literature that, apart from possessing several biological activities,

thiophenes are also useful intermediates for the synthesis of several chemical and pharmacological

classes of therapeutic agents having heterocyclic structures in them. Also a number of thiophenes

with novel substituents were earlier prepared in our laboratories. These thiophenes were endowed

with significant biological activities. In continuation of the previous works, some novel piperidino

thiophene have been synthesized and characterized by following modified Gewald synthesis.

Key Word: Schiff base, thiophenes, condensation, piperidine

PP-59

Biosensors in Cancer Diagnosis

Shilpi Srivastava, Ajay Kumar Singh and Atul Bhargava

Amity Institute of Biotechnology, Amity University Uttar Pradesh (Lucknow Campus), Gomti Nagar

Extension, Lucknow, UP 226028, India;

(CH3)2CHNH C

H2

CN

O

CH3COOH

NH4OOCCH

3

N

O

CH3

NCH

3

CONHCH(CH3)

2

CN

NCH

3S

NH

O

NH2

CH(CH3)

2

+Benzene

Refluxed for 09 hrs

,

Sulfur, 1 hr, 45-500C

Morpholine, ethanol




243


ABSTARCT

A biosensor is defined as a compact analytical device incorporating a biological or biologically-

derived sensing element either integrated within or intimately associated with a physicochemical

transducer. In 2012, 8.2 million deaths from cancer were reported worldwide and the number of

new cases is expected to rise by about 70% over the next 2 decades. Since cancer is caused by a

range of genetic and environmental factors, clinical testing of this disorder is also very complex.

Cancer biomarkers are considered as valuable tools for early detection of cancer, accurate

pretreatment staging, determining the response of the tumor to chemotherapy treatment, and

monitoring disease progression. Novel biomarkers based on proteins, peptides, gene mutations and

over/under expression of gene markers have been evaluated for cancer diagnosis. The emerging

field of biosensor technology has the potential to provide rapid and accurate results for cancer

diagnosis and therapy while maintaining cost effectiveness.

Key words: Cancer, Biomarkers, Disease diagnosis, Peptides

PP-60

NANOBIOTECHNOLOGY AND DRUG DELIVERY: NEW AVENUES

Shilpi Srivastava1,*, Atul Bhargava1 and Prashant Kumar Sharma2

1Amity Institute of Biotechnology, Amity University Uttar Pradesh (Lucknow Campus), Gomti Nagar

Extension, Lucknow, UP 226028, India

2DAV PG College, Dehradun

Corresponding author email: [email protected]

ABSTRACT

Nanobiotechnology is a multidisciplinary field that covers a diverse array of technologies from

biology, physics, chemistry, and engineering. Nanomedicine is the application of

nanobiotechnology in medical science to improve diagnosis as well as therapy. Nanomedical

devices can be applied for analytical, imaging, detection, diagnostic and therapeutic purposes and

procedures, such as targeted drug delivery, improving cell-material interactions and gene delivery

systems, and provide innovative opportunities in the fight against incurable diseases. The




244

development of a new generation of therapeutics has made drug delivery an important issue,

especially, for drugs which are either unstable in the biological environment, have poor transport

properties across biological membranes, are insoluble in water, or have very low bioavailability.

Different types of nano-sized carriers, such as nanowires, nanocages, nanoparticles and dendrimers

are in the process of being developed for various drug-delivery applications. Drug delivery

mediated by nanomaterials is still in the early stages of development; but, its development is

multidirectional and fast-paced with endless possibilities for new therapies to treat illness and

diseases.

Key words: Nanomaterials; Drug delivery; Disease diagnosis.

PP-61

Nanocarrier: An Effective Mean to Integrate Phytochemical for Enhanced

Bioavailabilty and Efficacy

Himani Awasthi

Amity Institute of Pharmacy, Amity University Uttar Pradesh, Lucknow Campus

ABSTRACT

Herbal medicine are widely and most easily available phytopharmacological product to treat

number of disease but the effectiveness of herbal product depends on supply of their active

constituent and their hydrophilic lipophilic value. Before entering to the systemic circulation,

many constituents of the herbal drugs will be degraded resulting less bioavailability in the highly

acidic pH of the stomach and other constituents might be metabolized by the liver. Nanocarriers

applying to herbal remedies will carry optimum amount of the drug to their site of action bypassing

all the barriers such as acidic pH of stomach, liver metabolism and increase the prolonged

circulation of the drug into the blood due to their small size

Another problem with phytochemicals is that most of the phytochemicals are easily soluble in

water but their bioavailability and efficacy is very less so they need repeated administration to

maintain the therapeutic level in plasma throughout the treatment schedule. To overcome this

problem one approach is nanotechnology based herbal product. Nanomaterial based

phytochemical has added advantage such as their unique small size and good absorption profile

and controlled release of drug. So, using herbal drug in the nanocarriers will increase its potential

for treatment of different chronic diseases and health benefits. Thus integration of nanocarrier with

phytochemicals has potential to enhance the efficacy, activities as well as bioavailability hence

overcome the problem associated with dosing of herbal drug.

PP-62


245

Preparation & Evaluation of Solid Lipid Nanoparticles of Norfloxacin for

Ocular Delivery

Wasim Khan,

Asst Prof BGI, Bulandsahr, UP

ABSTRACT

The aim of the present research work was to formulate solid lipid nanoparticle of Norfloxacinfor

ocular delivery. A modified solvent-displacement (nano-precipitation) technique & high speed

homogenization method were used to prepare biocompatible lipid nanoparticles(SLNs), stabilized

by ethanol The prepared nanoparticles were characterized for pH, particle size, surface

morphology, entrapment efficiency, in vitro release, ocular tolerance and stability. Surface

properties of the nanoparticles were studied by Scanning Electron Microscopy and nanoparticles

found to have smooth surface. SLN of antibacterial drug were prepared by high speed

homogenization method.Various formulation and process parameters were optimized to get

nanosized particles with maximum drug entrapment efficiency. Different parameters viz.

(surfactant and cosurfactant effects, surfactant and cosurfactant ratio,oil-surfactant ratio) involved

in the method were optimized, to obtain small nanoemulsion with maximum drug entrapment.

The principal objective of the present work was to make Norfloxacin formulation which is devoid

of hypersensitivity reaction and fluid retention thereby avoiding pre-medications. The

antibacterial drug Norfloxacin was formulated in the non-ionic surfactant Polysorbate-80 (Tween

80) & PEG with polymer PC/Eudragit RL-100. First, surfactant and cosurfactant, formulations

were prepared in which one of the composition has been omitted and other contents were kept

constant.In formulation N1,the surfactants (PC: Tween-80) and cosurfactants(PEG: Ethanol) were

taken in 1:1 ratio. In formulation N2, Tween-80 was omitted and other contents were kept constant

with same ratio as in F1.Informulation N3,PEG has been omitted, and other contents were constant

as informulation N1.The designed nanoparticles have average particle size from 278-441 nm and

zeta potential from 22 to -26 mV. Cumulative percent drug released for N-1 to N-6 after 12 hours

was 86.30 %, 84.73%, 79.97%, 74.62%, 73.17% and 72.19%respectively. Formulations show no

irritations in ocular tolerance test. The developed formulations were therapeutically efficacious,

stable, non-irritant and provided sustained release of the drug. Stability studies showed that 40˚C

is optimum temperature for storage of nanoparticles. From the experimental finding, it is

concluded that:

• Polymer Eudragit RL-100 is a promising agent for ocular delivery.

• Formulation N-4 showed maximum drug encapsulation efficiency.

• Formulations N-4 and N-5 showed maximum cumulative percent drug release.


246

• An increase in the amount of polymer to the formulations enhanced the drug entrapment

efficiency.

• The pH of all formulations was found to be satisfactory thus there would be no irritation to the

patient upon administration of the formulation.

Keywords: Nanoparticle; Norfloxacin; SLN, PEG=Phosphoenol pyruvate, PC=Phosphotidyl

choline

PP-63

Effect of Catharanthus and Lemon grasson the scavenging and redox system of

human blood platelets.

Ananya Mishra, Abhay Prakash Pandey, VineetAwasthi, Gurjeet Kaur.


ABSTRACT

Super oxide dismutase (SOD) is the most powerful naturally occurring antioxidant which prevent

damage to tissues. Platelets have been suggested to release super oxide dismutase. Also platelet

activation is thought to be a key event in acute vascular thrombosis. We target to find a way to

prevent platelet activation. Indian Ayurvedic medicines and other traditional herbal systems use

Catharanthusroseus for home remedies. The medicinal properties of the plants are well known for

their use in case of diabetes, gastro intestinal tract problems, etc.

Aim of this review is to find the effects of these medicinal plants on human blood platelets

(synergistic or antagonistic). For this level of SOD was determined in extracts of plants at 480 nm

also level of protein was determined in extracts of plants by Bradford’s method , level of

malondialdehyde (MDA) was determined through lipid peroxidation. The synergistic effect of

medicinal plant extracts and human blood platelets may have a crucial role in treatment of ischemic

heart disease condition.

PP-64

In-Vitro Free Radical Scavenging and Total Antioxidant Potential of Crotalaria

juncea L. seeds


247

Jamal AkhtarAnsari1,2,Abbas Ali Mahdi2 , Mohammad Kaleem Ahmad2 , Homa Jilani Khan1,2, Nishat

Fatima1,2, Murtaza Abid2 , Abdul Rahman Khan1*

1Department of Chemistry, Integral University, Lucknow-226026, U.P., India 2Natural Product Research

Lab, Department of Biochemistry, King George’s Medical University, Lucknow- 226003, U.P., India


ABSTRACT

Crotalaria juncea L. known as Sunn or Sunn hemp is a tropical Asian plant of the legume family

(Fabaceae). Traditionally it is used for the treatment of anaemia, impetigo, menorrhagia, psoriasis.

In our medicinal plants screening program at natural product research lab we have evaluated C.

juncea (Fabaceae) seeds for the antioxidant potential by evaluating the Total Antioxidant Capacity

(TAC), and inhibition to 2, 2-diphenyl-1-picryl-hydrazyl (DPPH) free radical. Among different

fractions, petroleum ether (CJPE), chloroform (CJC), methanolic fractions (CJM) and aq.

methanolic (CJAM), methanolic fraction showed highest TAC with 1000 µg of extract equivalent

to 1.6 µg/ml ascorbic acid, consequently CJC and CJAM demonstrated 1.5µg/ml and CJPE with

lowest 1.1 µg/ml value. Inhibition of DPPH free radical revealed that from a concentration of

400µg/ml to 1000 µg/ml ofdifferent extracts inhibits 14.18% to 14.46 % for CJPE, 16.13% to

23.64 % for CJC, 30.45% to 69.68% for CJM and 46.59% to 85.53% for CJAM. The IC50 value

was obtained lowest for CJAM (455 µg/ml) as compared with CJM (705 µg/ml) however, CJPE

and CJC corresponded to a higher dose. The study demonstrated that different fractions of C.

juncea seeds have potential to inhibit free radical. Moreover, among all the fractions aq.

methanolic fractions (CJAM) and methanolic (CJM) have significant antioxidant activity.

Therefore, further in-depth studies are warranted to explore its active principles. Furthermore,

seeds of C. juncea can be used as natural antioxidant in herbal formulation.

Keywords: Total Antioxidant Capacity, DPPH, Crotalaria juncea, Antioxidant.

PP-65

Evaluation of In-Vitro Antioxidant Activity of Anthocephalus cadamba (roxb.)

Miq Bark Fractions

Nishat Fatima1,2, Abbas Ali Mahdi1 , Jamal AkhtarAnsari1,2, Mohammad Kaleem Ahmad2 , Homa Jilani

Khan1,2, Abdul Rahman Khan1 , Zulfiqar Ali2*

1Department of Chemistry, Integral University, Lucknow-226026, U.P., India 2Natural Product Research

Lab, Department of Biochemistry, King George’s Medical University, Lucknow- 226003, U.P., India




248

ABSTRACT

Objectives: The aim of the study was to evaluate the antioxidant activity of different fractions of

Anthocephalus cadamba bark.

Methods: A. cadamba bark different fractions hexane, chloroform, methanol and aqueous

alcoholic were screened for antioxidant activity by the use of Total Antioxidant Capacity by

phosphomolybdenum method and DPPH Radical scavenging activity in a concentration dependent

manner. The ascorbic acid was used as reference standard.

Results: TAC of different fractions (1000 µg/ml) were found to 2.0 µg/ml, 1.7 µg/ml, 1.2 µg/ml

and 0.9 µg/ml equivalent to ascorbic acid for hexane, chloroform, methanol and aq. alcoholic

fractions, respectively. The percent inhibition of DPPH free radical values of hexane, chloroform,

methanol and aq. alc. fractions were 13.90%, 51.58%, 59.41%, 54.23% and 52.46%, respectively.

The scavenging effect of various fractions based on their IC50 values was in the order of methanol

(675 µg/ml) > aq. alc. (745 µg/ml) > chloroform (815 g/ml). The results were compared with

ascorbic acid as reference standard (IC50=0.680 µg/ml).

Conclusion: The results obtained showed that the bark of A. cadamba have potent antioxidant

properties. Therefore, it can be considered as good source of natural antioxidant and can be

incorporated into the drug formulations.

Keywords: A. cadamba, Antioxidant, DPPH, TAA.

PP-66

Evaluation of Antioxidant Potential of Swertia Chirayata L.

Homa Jilani Khan1,2,Abbas Ali Mahdi2 , Jamal Akhtar Ansari1,2, Mohammad Kaleem Ahmad2 , Nishat

Fatima1, 2, Abdul Rahman Khan1 *

1Department of Chemistry, Integral University, Lucknow-226026, U.P., India

2Natural Product Research Lab, Department of Biochemistry, King George’s Medical University,

Lucknow- 226003, U.P., India


ABSTRACT



249

Objectives In the present study the antioxidant potential of traditional Indian medicinal Swertia

chirayata (Gentianaceae) has been evaluated.

Methods Different fractions in hexane, chloroform, methanol and aq. methanol of aerial part of S.

chirayata (Gentianaceae) were prepared. Antioxidant activity of fraction was evaluated by Total

Antioxidant Activity (TAA) based on phosphomelybdenum reduction, DPPH (1, 1-diphenyl-2-

picrylhydrazyl) scavenging radical activity.

Results S. chirayata showed that TAA 1000 µg/ml fractions equivalent to ascorbic acid; 3.3 µg/ml,

3.3 µg/ml, 1.4 µg/ml and 1.5 µg/ml for hexane, chloroform, methanol and aq. methanol,

respectively. However, DPPH inhibition was 0.39 to 3.57% for hexane, chloroform 1.7% to 5.03%,

methanol showed 0.79% to 59.86% and aq. methanol was 0.26 to 7.81. The IC50=value was

obtained 1240 µg/ml for methanolic fraction, however, other fractions values were at higher

concentration.

Conclusion On the basis of above result it can be concluded that S. chirayta has potential to inhibit

free radical. Moreover, among all fractions methanolic fractions was more potential as compared

with others. In conclusion, further studies are warranted to identify its bioactive principles.

Keywords: Swertia chirayta, Antioxidant, DPPH, TAA.

PP-67

Therapeutic potential of Thymoquinone: An active phytochemical of Nigella

sativa

MohammedShariq Iqbal, Mohammad Israil Ansari and Brijesh Pandey#

Amity Institute of Biotechnology, Amity University Uttar Pradesh, Lucknow Campus, U.P, India.

#corresponding author; E-Mail: [email protected], [email protected]

ABSTRACT

Thymoquinone (2-Isopropyl-5-methylbenzo-1,4-quinone, molecular formula C10H12O2)is an

active phytochemical found in the plant Nigella sativa. Thymoquinone has been experimentally

validated to have therapeutic significance. It has been an antioxidant, analgesic, anticonvulsant

and angiogenesis inhibitory effects and has been shown to protect against heart, liver and kidney

damage in animal studies as well as having possible anti-cancer effects. Thymoquinone has been

shown to have effect on immune response by controlling dendritic cell functions such as oxidative

burst, cytokine release, cell pH and maturation.Molecular mechanism ofits action and its capability

to induce apoptosis and restrain tumor growth is experimentally observed. Thymoquinoneis also






http://en.wikipedia.org/wiki/Molecular_formula



http://en.wikipedia.org/wiki/Antioxidant

http://en.wikipedia.org/wiki/Analgesic

http://en.wikipedia.org/wiki/Anticonvulsant

http://en.wikipedia.org/wiki/Angiogenesis_inhibitor


250

reported for its anti-inflammatory effects, it inhibits tumor cell propagation through inflection of

apoptosis signaling, and cell cycle arrest, with inhibition of angiogenesis. There have been efforts

to amalgamate novel analogs of thymoquinoneheading in the direction of betterproperty in killing

tumor cells with more improvedchemosensitizing potential than presentthymoquinonecompound.

Based on earlier studies, we believe that morein detail studies are necessary and explorationof its

bioavailability and toxicity in human subjects is imperative.

PP-68

Folate — a double-edged sword in cancer

Apeksha Srivastava, S. Marzia Ali, Lavie Rekhi, Sayali Mukherjee, Somali Sanyal, Sonia Chadha

Amity Institute of Biotechnology, Amity University, Lucknow Campus

ABSTRACT

Folic acid, a member of the vitamin B complex familycannot be synthesized but is obtained from

diet, primarily through fruits, vegetables, and fortified grains. Folic acid is enzymatically reduced

in vivoto tetrahydrofolate by dihydrofolatereductase which is involved in one carbon metabolism.

Tetrahydrofolate is required for the de novo synthesis of thymidylate and purinesnucleotides that

are needed for DNA replication and repair. Folatemetabolites are also utilized in the conversion

of homocysteine to the amino acid methionine and its subsequent conversion to S-

adenosylmethionine (SAM or SAdoMet). SAM plays an important role in DNA methylation and

hence, in gene regulation.Metabolism offolatehas been shown to play a dual role in cancer.

Inadequate folate intake is associated with DNA damage and altered DNA methylation which

may lead to malignant transformation. On the other hand inhibition of folic acid metabolism

hasalso been used as a mechanism for elimination of malignant cells. Folate intake before the

development of preneoplasticlesions can prevent tumor development, but, supplementation with

synthetic folic acid may enhance progression once preneoplastic lesions are present. These

opposing effects are due to the role of folate in the nucleotide metabolism in both normal and

malignant cells. Thus there is a need to study in detail the role of folate and its metabolism in

relation to cancer.

Keywords: Folate, cancer, tetrahydrofolate, DNA damage and repair

PP-69

Review on Techniques for Enhancement of Solubility of Statins

Richa Srivastava, Sadaf Zaidi, Devdutt Chaturvedi.


251

Amity Institute of Pharmacy, Amity University, Lucknow Campus, Uttar Pradesh

e-mail :- [email protected]

ABSTRACT

Statins are significant to the researchers because of their significant capability to act as drug

delivery vehicles by incorporating an extensive range of drug molecules. The present

communication embodies approaches in the design of lipid based formulation, evaluation

processes, mechanism involved there in, updated with latest findings from literature reports and

patents. This all-inclusive review offers an overt discussion on bioavailability improvement of

various drugs in gastrointestinal (GI) media. About 40% of drugs are not soluble in water in

practice and therefore are slowly absorbed, which consequences in inadequate and rough

bioavailability and GI toxicity. Thus, most difficult phase of drug development practice

particularly for oral dosage forms is the improvement of drug solubility and thereby it’s oral

bioavailability.

Various trials have been successfully employed to improve solubility for bioavailability

enhancement; yet, successful improvement essentially depends on the assortment of technique.

This evaluation describes various conventional and novel methodologies anticipated for solubility

enhancement of Statins, and eventually improvement in its bioavailability thus encouraging the

researchers to accelerate their research work in this direction for the development and enhancement

of dissolution profile of hydrophobic drugs and shell out a novel advance en route for

pharmaceutical research.

Keywords: techniques, absorption, bioavailability

PP-70

Folate Targeted (Nano) Drug Delivery Systems Using Folate as a Targeting

Ligand.

Richa Srivastava, Sadaf Zaidi, Devdutt Chaturvedi.


e-mail: [email protected]

ABSTRACT

Folate targeted drug delivery has emerged as an unconventional therapy for the management and

imaging of many cancers and inflammatory diseases. Folate conjugates can deliver a variety of

molecular complexes to pathologic cells due to their small molecular size and high binding affinity


252

for cell surface without causing harm to normal tissues. It involves the attachment of the vitamin,

folate (folic acid), to a molecule/drug to form a "folate conjugate".

As cancer cells require excessive folic acid, which is a ligand for folate receptors, to enable their

rapid proliferation, thus to target these excessively proliferating cells, conjugates of folic acid

havebeen used for targeted delivery of radionuclides, oligonucleotides , and drugs cells, where

these conjugates enter cells via folate receptor-mediated endocytosis.

The smartly engineered nanoparticles have confirmed enormous potential as cellular drug delivery

vehicles. They improve drug's stability as well as its bioavailability and retention at the targeted

site of action .The conjugated ligand to nanoparticle surface have enhanced therapeutic efficacy

and it also modifies the intracellular disposition of nanoparticles. Thus, this review aims at

providing a brief overview of Folate Receptor targeting in drug delivery, with an emphasis on the

strategy of using folate as a targeting ligand.

KEYWORDS: Therapeutic Efficacy, Folate targeted drug delivery, Radionuclides.

PP-71

Development of Nano-Self Emulsifying Drug Delivery System for Antimalarial

Treatment.

Richa Srivastava, Pankaj Dwivedi,2 A.K.Dwivedi2

1Amity Institute of Pharmacy, Amity University, Lucknow Campus, Uttar Pradesh

2.Pharmaceutics Division, CSIR-CDRI, Lucknow.

e-mail :[email protected]

ABSTRACT

-Arteether, an effective artemisinin derivative, is used in the treatment of malaria but is available

only as an intramuscular injection. Due to its low aqueous solubility and low permeability,

dissolution and/or release rate from the delivery system forms the rate limiting step in its

absorption and systemic availability. For the therapeutic delivery of lipophillic active moieties

(BCS class II drugs), lipid based formulations are inviting increasing attention. Currently a number

of technologies are available to deal with the poor solubility, dissolution rate and bioavailability

of insoluble drugs , one of them is Self-Micro Emulsifying Drug Delivery Systems (SMEDDS).

Thus, the objective of the present investigation was to formulate self-micro-emulsifying drug

delivery systems (SMEDDS) using Lauroglycol 90, Labrasol, Labrafac PG, Groundnut Oil as an

oily phase. SMEDDS based on lipophillic phase and cremephor EL were formulated using ternary


253

phase diagrams and were applied in improving the delivery of a lipophilic anti-malarial drug, -

arteether. The prepared formulations were characterized with respect to mean globule size and in

vitro drug release profile. The in vivo anti-malarial performance of the developed SMEDDS was

evaluated in Sprague Dawley rats infected with strain of Plasmodium. In 250 ml of simulated

gastric medium, 1 g of these SEDDS solubilized the daily dose of -arteether and formed lipid

droplets of average size 80–250 nm. The other parameters studied were HPLC Analysis of Drug,

Infrared Spectrum, HPLC Analysis of Drug at various pH for stability, Differential Scanning

Colorimetry (DSC),Thermodynamic stability studies, Droplet Size Analysis ,Zeta Potential

Measurements ,In vitro Diffusion Study ,Stability study by HPLC and Zeta Potential

Measurements, activity against time and animal survival period.

SMEDDS showed excellent self-micro-emulsification efficiency and released >92% of the drug

in 24 hrs.The stability of the micro-emulsion was evaluated at 5o C and 40o C for 1 month. The

anti-malarial studies revealed that SMEDDS resulted in significant improvement in the anti-

malarial activity .The developed SMEDDS highlight safety for use and potential applications of

Self-emulsifying drug delivery systems which substantially improved solubility/dissolution,

absorption and bioavailability of poorly water-soluble anti malarial drug, -arteether.

Keywords: b-arteether, poor water solubility, micro-emulsion, parenteral delivery

PP-72

Organogels: Trending Novel Drug Delivery System.

Rahul Kushwaha*,Ankan Rastogi, Richa Srivastava, Devdutt Chaturvedi.


E-mail :- [email protected]

Organogel, is a non crystalline, non-glassy thermosreversible (thermolastic) solid materials

and viscoelastic system, can be regarded as a semi-solid preparation which has an immoblized

external a polar phase. A gel may be defined as semi-solid formulation having an external solvent

phase apolar (organogel) or polar (hydrogel) immoblized within the spaces available of a three

dimensional networked structure. The organogel do not form semisolids on standing because an

organogel may consist of macromolecules existing as twisted matted strands. The units are bound

together by strong types of vander-Waal forces so as to form crystalline amorphous regions. Gels

can also be classified according to the bonds present in the gelator network: physical gels are held

by weaker physical forces of attraction such as vander-Waals interactions and hydrogen bonds,

whereas chemical gels are held by covalent forces. Often, these systems are based on self assembly

of the structrant molecules. In general, organogel are thermodynamically stable in nature and have

been explored as matrics for the delivery of bioactive agents, organogels have potentials of use in


254

number of applications, such as in pharmaceuticals, cosmetics, art conservation and food. It can

also be used for drug and vaccine delivery via different administration routes, although relatively

few such formulations have investigated only a few organogels have been investigated for drug

delivery despite the very large number of organogels under study. An example of formation of an

undesired thermoreversible network is the occurrence of waxy crystallization in petroleum. In the

current manuscript, an attempt has been made to understand the properties of organogels, various

types of organogelators and some applications of the organogels in controlled delivery.

PP-73

Liposomes: An Advancement in Novel Drug Delivery systems

Nishita Singh, Komal Agarwal, Sumit Bajpai, Richa Srivastava

Amity Institute of Pharmacy, Amity University, Lucknow Campus.

ABSTRACT

The discovery of liposome or lipid vesicle emerged from self forming enclosed lipid bi-layer upon

hydration. Liposome drug delivery systems have played a significant role in formulation of potent

drug to improve therapeutics. Recently the liposome formulations are targeted to reduce toxicity

and increase accumulation at the target site. There are several new methods of liposome

preparation based on lipid drug interaction and liposome disposition mechanism including the

inhibition of rapid clearance of liposome by controlling particle size, charge and surface hydration.

Most clinical applications of liposomal drug delivery are targeting to tissue with or without

expression of target recognition molecules on lipid membrane. The liposomes are characterized

with respect to physical, chemical and biological parameters. The sizing of liposome is also critical

parameter which helps characterize the liposome which is usually performed by sequential

extrusion at relatively low pressure through polycarbonate membrane (PCM). This mode of drug

delivery lends more safety and efficacy to administration of several classes of drugs like antiviral,

antifungal, antimicrobial, vaccines, anti-tubercular drugs and gene therapeutics. Current

applications of the liposomes are in immunology, dermatology, vaccine adjuvant, eye disorders,

brain targeting, infective disease and in tumour therapy and as carriers for hydrophilic (water

soluble) anticancer drugs like doxorubicin, mitoxantrone; and bisphosphonate-liposome mediated

depletion of macrophages. This review would be a help to the researchers working in the area of

liposomal drug delivery.

PP-74

Role of Community Pharmacist in Healthcare of the Society

Abhishek Nayak, Richa Srivastava, Devdutt Chaturvedi.


255

Amity Institute of Pharmacy, Amity UniversityUttar Pradesh, Lucknow Campus

ABSTRACT

Community pharmacists are the health professional most accessible to the public after Doctors.

Community pharmacists are those who supply medicines in accordance with a prescription or

when legally permitted, or sell them without a prescription. Community pharmacists play a vital

role in the healthcare of the society. Indian Pharmacists have also progressively under taken the

additional task of ensuring the quality of the product they supply to the sick.

The contribution of pharmacists to health care is based in most countries upon a body of

knowledge and expertise acquired from a university degree. Community Pharmacists also have an

indisputable function at varied levels in national drugs registration and regulation. Pharmacists

understand and ensure the principle of quality assurance as they are applied to medicines.

Pharmacists are also responsible for the pricing structure applied to medicinal products.

Community Pharmacists collect and interrogate information about the patient, drug, history, verify

the patient understanding of the intended dosage regimen and method of administration and

advises the patient of drug related precautions. Pharmacists can compile and maintain information

on all medicines and particularly an newly introduced medicines, provide this information as

necessary to other healthcare professionals. Community Pharmacists also give the information

about diseases in the healthcare.

PP-75

An efficient, one-pot, syntheses of trithiocarbonates through corresponding

alkyl halides employing Cs2CO3/CS2 System

Nitin Srivastava,bSadaf Zaidi,a,b Amit K. Chaturvedi,cDevdutt Chaturvedi,a,*



b Amity School of Applied Sciences, Amity University Uttar Pradesh (AUUP), Lucknow Campus,


cSynthetic Research Laboratory, Department of Chemistry, B. S. A. P. G. College, Mathura-281004, U.

P., India


Abstract:




256

Dialkyltrithiocarbonates are very important class of compounds have frequently been used as

agrochemicals and lumbricating additives, dibenzyltrithiocarbonates (DBTTC) derivatives are

focused as reversible addition fragmentation chain transefer (RAFT) agent. Thus, a facile synthesis

of trithiocarbonates is desired in order to attain the efficient production. Classical synthesis of

trithiocarbonates involves reactions of thiols with either thiophosgene or chlorodithioformates, and

two-step reactions of thiols with carbon disulfide and alkyl halides under basic conditions. These

reactions however, must employ highly toxic chemicals with unpleasent odors. Another general

method for trithiocarbonates is the dialkylation of thrithiocarbonate anion with alkyl halides using

phase transefer catalysts or at elevated temperatures (70oC). This dialkylation is also inconvenient,

because it requires 10 to 19 fold molar excess amount of carbon disulfide and bases toward alkyl

halides. The toxicity and bad smell of CS2 result in that the use of minimum amount of carbon

disulfide is desirable for more efficient and sustainable synthesis of trithiocarbonates embark on

the improved procedures. Thus, we were prompted to embark on the improved procedures. Our

group has been engaged from the past several years for the development of new and efficient

protocols for the synthesis of carbamates, dithiocarbamates, dithiocarbonates (xanthates) using

cheap and abundantly avaliable reagent like CO2 and CS2 respectively. In the present

communication, we report here an efficient and novel protocol for the preparation of the

symmetrical trithiocarbonates from the corresponding alkyl halides using minimum amount of

Cs2CO3/CS2 system (Scheme 1).

R2

R1

R3

X2 R2

R1

R3

S S

S

R1

R3

R2

Scheme I

dry DMSO, Cs2CO3, CS2

RT, 3-6h, 80-99% yields

X = Cl, I, Br

References:

(a) D. Chaturvedi,* et al, Tetrahedron Lett.2003, 44, 7637.(c) Tetrahedron Lett.2006, 47, 1307.

(d)Tetrahedron Lett.2007, 48, 149. (e)Tetrahedron Lett.2007, 48, 5043.; (f)Synthesis2008, 355-

357; (g) TetrahedronLett.2008,49, 4886-4888; (h) )Tetrahedron Lett.,2012,53, 5398-5401;(i)

Tetrahedron,2012,68,15-45; (j)Synlett.,2012, 23, 2627-2630; (k) Org. Biomol. Chem.,2012,10,

9148-9151; (l) Synlett.,2013, 24, 33-36

PP-76

Dithiocarbamates of ω-substituted (2-naphthyloxy) alkanes: A novel class of

potential antioxidant agents

Sadaf Zaidi,a,b Richa Srivastava,a Amit K. Chaturvedi,c Gaurav Kaithwas,c Devdutt Chaturvedi,a,*


257



bAmity School of Applied Sciences, Amity University Uttar Pradesh (AUUP), Lucknow Campus,


*Corresponding author’s e-mails:[email protected], [email protected]

ABSTRACT

Dithiocarbamateis a key structural unit in various fields like pharmaceuticals, agrochemicals,

intermediates in organic synthesis, protection of amino group in peptide chemistry, combinatorial

chemistry, and ligand for soft metal complexation, synthesis of nanoparticles, synthesis of ionic

liquids and as useful synthon in organic chemistry.As a potential versatile synthon,

dithiocarbamates have been utilized for the synthesis of structurally diverse biologically potent

compounds like isothiocyanates, thioureas, cynamide, dithiobenzophene, glycosides, amide and

heterocyclic compounds. Furthermore, the role of the dithiocarbamate linkage has been

extensively studied in structurally diverse natural/semisynthetic molecules against various

diseases such as anticancer, antibacterial, antifungal, antimalarial, antiviral, anti-HIV,

antiestrogenic, antiprogestational, antiosteoporosis, antiinflammatory, antifilarial, antitubercular,

antidiabetic, antiobesity, anticonvulsant, antihelminthes, anti-alzheimer drugs, and CNS and CVS

active agents In recent years, researchers around the globe are emphasizing on antioxidant activity

of natural/semisynthetic/synthetic dithiocarbamates. In continuation with our research work upon

the synthesis and bioevaluation of dithiocarbamates, we have synthesized a novel series of

dithiocarbamates of ω-substituted (2-napthaloxy) alkanes Iand investigated their antioxidant

activity. Interestingly, majority of them have shown promising antioxidant activity as compared

to sample drugs which we will represent in our presentation.

O

S

S

N

prototype IR2

R1

n

References:

Chaturvedi, D.* et al.TetrahedronLett.2003, 44, 7637-7639; (b) TetrahedronLett.2006, 47, 1307-

1309; (c) Tetrahedron Lett.2007, 48, 149-151; (d) Tetrahedron Lett.2007, 48, 5043-5045; (e)




258

Synthesis 2008, 355-357; (f) Tetrahedron Lett.2008, 49, 4886-4888; (g) Curr. Org.

Chem.,2011,15, 1593-1624; (h) Tetrahedron Lett.,2012,53, 5398-5401;(i) Tetrahedron,2012,68,

15-45; (j) Curr. Org. Chem.,2012,16, 1609-1635; (k) Synlett.,2012, 23, 2627-2630; (l) Org.

Biomol. Chem.,2012,10, 9148-9151; (m) Synlett.,2013, 24, 33-36.

PP-77

An efficient method for the synthesis of substituted-1,3-oxazolidine-2,4-diones through the

corresponding haloamides using Triton-B/CO2 system

Amit K. Chaturvedi,a,b Devdutt Chaturvedi,*,c and Virendra Mishraa

aSynthetic Research Laboratory, Department of Chemistry, B. S. A. P. G. College, Mathura-281004, U.

P., India

bDepartment of Chemical Sciences, GLA University, Mathura-281406, U. P

cDepartment of Chemistry, Amity School of Science and Technology, Amity University Uttar Pradesh


ABSTRACT

Substituted 1,3-oxazolidine-2,4-diones are biologically active compounds which finds use

as anti-convulsants, particularly interesting therapeutic properties were found in trimethadione

(3,5,5-trimethyl oxazolidine-2,4-diones), paramethadione (5-ethyl-3,5-dimethyl oxazolidine-2,4

diones) and malidone (3-allyl-5-methyl oxazolidine-2,4-dione). Several compounds belonging to

this class have displayed remarkable herbicidal activity. These compounds have been found as

useful synthon for the synthesis of biologically potent derivatives such as substituted α-hydroxy

carboxamides, substituted α-hydroxy hydrazides etc. Their traditional syntheses involved the use

of harmful reagents such phosgene, its derivatives and carbon monoxide or isocyanates. Recently,

carbon dioxide has only been used as a cheap and safe alternative in the synthesis of substituted

1,3-oxazolidine-2,4-diones employing the electrochemical form of carbon dioxide using various

kinds of starting materials and reagents/catalytic systems. Moreover, their formation using CO2

employed harsh reaction conditions such as higher reaction temperatures, longer reaction time and

tedious workup. Therefore, we would like to embark on the developments of improved procedures

for the synthesis of substituted 1,3-oxazolidine-2,4-diones employing gaseous carbon dioxide as a

source of carbonyl functionality. Our group6 has been engaged over several years on the

development of new and efficient and safer protocols for the synthesis of carbamates,

dithiocarbamates, dithiocarbonates (xanthates) using cheap and abundantly avaliable reagent like

CO2 and CS2 respectively. In the present paper, various kind of substituted-1,3-oxazolidine-2,4-

diones Ihave been synthesized through their corresponding haloamides employing Triton-B/CO2

System (Scheme 1).


259

O

OR1

NHR3

O

X

R1

NO

Dry DMSO, Triton-B

R3

X = leaving group, i.e. halides (Cl, Br, I )

R1 = R2 = alkyl/aryl/ heteroaryl and its substituted derivatives

R2

CO2, 60oC, 2-3.5h

Substituted haloamides

R3 = alkyl/aryl/cycloalkyl/naphthyl/substituted aryl/heteroaryl

R2

80-98%

123

1

2

3

45

I

Scheme 1

PP-78

An efficient method for the syntheses of β-substituted alkyl carbamates through

the Michael addition approach

Sadaf Zaidi,a,cAmit K. Chaturvedi,b Pragyandeep P. Dash,a Devdutt Chaturvedi,a,*



bDepartment of Chemistry, GLA-University, Mathura-281004, U. P., India

cAmity School of Applied Sciences, Amity University Uttar Pradesh (AUUP), Lucknow Campus,



ABSTRACT

Organic carbamates considered as magical compounds holds unique applications in the field of

pharmaceuticals, agrochemicals (pesticides, herbicides, insecticides, fungicides etc.), and

intermediates in organic synthesis, for the protection of amino groups in peptide chemistry, as

linkers in combinatorial chemistry etc. Organic carbamates have been extensively used as useful

synthons for the synthesis of structurally diverse synthetic intermediates/molecules of biological

significance. Organic carbamates have frequently been employed as demandable pharmaceuticals

in the forms of drugs and prodrugs. In recent years, several reports have indicated that carbamate

linkage present in between the active pharmacophores of various structurally diverse molecules




260

increases manifold biological activities of semisynthetic/synthetic natural/synthetic molecules. To

satisfy their demand, their synthesis has been changed from the use of costly and toxic chemicals

such as phosgene and its derivatives directly or indirectly, to the abundantly available cheap and

safe reagents like CO2. Moreover, their formation by using CO2 employed harsh reaction

conditions such as use of strong bases, higher reaction temperatures and longer reaction times. Our

group has been engaged from past several years for the development of new methodologies for the

preparation of carbamates, dithiocarbamates and related compounds using cheap, abundantly

available, and safe reagents like CO2 and CS2 respectively. Recently, we found that Triton B is the

best catalyst for the synthesis of carbamates, dithiocarbamates, carbazates, dithiocarbazates,

dithiocarbonates (xanthates) employing a variety of reagents and catalytic systems. In the present

paper, we report herein a new and efficient one-pot method for the synthesis of β-substituted alkyl

carbamates through the Michael addition reaction of carbamate anion to the α,β-unsaturated

carbonyl compounds employing catalytic amount of Triton-B at room temperature (Scheme 1). To

the best of our knowledge, this is the first report for the efficient and mild synthesis of β-substituted

alkyl carbamates employing Triton-B, afforded good to excellent yields (80-98%).

R1

NH

R2

+ +EWG

O

R

EWG

O

R

ON

O

R1

R2

CO2Dry DMSO, Triton-B

Scheme I

rt, 2-4h, 80-98%

References:(a) D. Chaturvedi,* et. al, Tetrahedron Lett.2003, 44, 7637-7639; (b)Tetrahedron

Lett.2006, 47, 1307-1309; (c) Tetrahedron Lett.2007, 48, 149-151; (d) Tetrahedron Lett.2007, 48,

5043-5045; (e) Synthesis 2008, 355-357; (f) Tetrahedron Lett. 2008, 49, 4886-4888; (g)

)Tetrahedron Lett., 2012, 53, 5398-5401; (h) Tetrahedron, 2012, 68, 15-45; (i) Synlett.,2012, 23,

2627-2630; (j) Org. Biomol. Chem.,2012,10, 9148-9151; (k) Synlett.,2013, 24, 33-36

PP-79

Insecticidal activity of dithiocarbamates of ω-substituted (2-naphthyloxy)

alkanes

Sadaf Zaidi,a,c Amit K. Chatuirvedi, Apeksha Srivastava,b S. Marzia Ali,b Lavie Rekhi,b J. K. Srivastva,b

Devdutt Chaturvedi,a,*


(AUUP), Lucknow Campus, Lucknow-226028, U. P. b Amity Institute of Biotechnology, Amity University Uttar Pradesh (AUUP), Lucknow Campus, Lucknow-

226028, U. P.


261

c Amity School of Applied Sciences, Amity University Uttar Pradesh (AUUP), Lucknow Campus,


*Correspondence, e-mails: [email protected], [email protected]

ABSTRACT

Dithiocarbamatesare intensively used in various fields like pharmaceuticals, agrochemicals,

intermediates in organic synthesis, protection of amino group in peptide chemistry, combinatorial

chemistry, and ligand for soft metal complexation, synthesis of nanoparticles, synthesis of ionic

liquids and as useful synthon in organic chemistry. As a potential versatile synthon

dithioarbamates have been utilized for the synthesis of structurally diverse biologically potent

compounds like isothiocyanates, thioureas, and cynamide, dithiobenzophene, glycosides, amide

and heterocyclic compounds. Furthermore, the role of the dithiocarbamate linkage has been

extensively studied in structurally diverse natural/semisynthetic molecules against various

diseases such as anticancer, antibacterial, antifungal, antimalarial, antiviral, anti-HIV,

antiestrogenic, antiprogestational, antiosteoporosis, antiinflammatory, antifilarial, antitubercular,

antidiabetic, antiobesity, anticonvulsant, antihelminthes, anti-alzheimer drugs, and CNS and CVS

active agents. In recent years, researchers around the globe are investigating

natural/semisynthetic/synthetic dithiocarbamate as agrochemicals. Various dithiocarbamate

bearing agrochemicals which are being actively used are mancozeb, maneb, propineb, ziram,

amobam, azithiram, carbamorph, ferbam, metam, nabem, tecoram and thiram. In continuation with

our research work upon synthesis and bioevaluation of dithiocarbamates, we have synthesized a

novel series of ω-substituted (2-napthaloxy) dithiocarbamates and investigated their insecticidal

activity. Interestingly, majority of them have shown manifold insecticidal activity as compared to

sample agrochemicals.

References:

Chaturvedi, D.* et al.TetrahedronLett.2003, 44, 7637-7639; (b) TetrahedronLett.2006, 47, 1307-

1309; (c) TetrahedronLett.2007, 48, 149-151; (d) TetrahedronLett.2007, 48, 5043-5045;

(e)Synthesis2008, 355-357; (f) TetrahedronLett.2008,49, 4886-4888; (g) Curr. Org.

Chem.,2011,15, 1593-1624; (h) Tetrahedron Lett.,2012,53, 5398-5401;(i) Tetrahedron,2012,68,

15-45; (j) Curr. Org. Chem.,2012,16, 1609-1635; (k) Synlett.,2012, 23, 2627-2630; (l) Org.

Biomol. Chem.,2012,10, 9148-9151; (m) Synlett.,2013, 24, 33-36.

PP-80

Molecular interaction of Survivin and naturally occurring ligands by In Silico

analyses for retinoblastoma targeting

Ajita Trivedi1, Anshul Tiwari1,2, Prachi Srivastava1*

1. AMITY Institute of Biotechnology, AMITY University Uttar Pradesh, Lucknow




262

2. Dept. of Ophthalmology, King George’s Medical University, Lucknow

*[email protected]

ABSTRACT

Retinoblastoma (RB) is a malignant tumor of the retina that most often occurs in children ages (0-

14). One naturally occurring cellular process that may accomplish induction of cell death is

apoptosis. Apoptosis, or programmed cell death, is an essential cellular process that is vital to

tissue development and homeostasis. However, in cancer cells, apoptosis is often evaded,

permitting the proliferation of malignant cells. One way that cancer cells elude apoptosis is by

manufacturing proteins known as Inhibitors of Apoptosis. One such inhibitor is a protein named

Survivin. Survivin inhibits caspases (proteases that carry out cell destruction within the apoptotic

pathway) thus preventing the commencement of cell death. Survivin is of research interest because

of its selective expression in cancer cells and absence in non-cancerous cells. The study was

undertaken in order to identify the experimental feasibility of Survivin inhibitor herbal ligands as

targeting treatment of Retinoblastoma. In this study, naturally occurring ligands was assessed for

its interaction with Survivin protein. Through molecular interaction studies with the available 3D

structure of Survivin, Ginkagolide was found to be the most potential ligand against

retinoblastoma. This study confers that Ginkgolide can be a good measure as on prophylactic

approaches against retinoblastoma.

Key Words: Retinoblastoma, Survivin, Molecular Interaction, In silico, Ginkgolide.

PP-81

Synthesis and anti-inflammatory activity of pyrazole based compound

Praveen Singh, Ashish Kumar Tewari

Department of Chemistry, Faculty of Science, Banaras Hindu University, Varanasi 221005

Email ID: [email protected]

The Non-steroidal anti-inflammatory drugs (NSAIDs) are a class of compounds used for the

treatment of pain, fever and inflammation, particularly arthritis by virtue of their analgesic and

anti-oedema properties.1,2 Many non-steroidal anti-inflammatory drugs (NSAIDs) were found to

interact with these enzymes and inhibit their enzymatic activity.3,4 COX-2 expression is induced

in a number of cells by pro-inflammatory stimuli and by cytokines. Traditionally suppression of

prostaglandin biosynthesis from arachidonic acid by inhibiting cyclooxygenases (COXs), by

Nonsteroidal anti-inflammatory drugs (NSAIDs).5-8There are large number of drugs are reported

in Pyrazolone moieties. This is mainly due to the easy preparation and the important versatile

biological activity. Pyrazolones are an active moiety in the class of NSAIDs and used in the



263

treatment of arthritis, musculoskeletal and joint disorder. Pyrazoles and its derivatives (1-6)

showed potent anti-inflammatory activity as examined by in silico (Figure 1) and in vivo studies.10

Scheme 1.Synthesis of ethylene and propylene linked phthalimide substituted pyrazole derivatives

Figure 1. Docked pose of compound 4 within COX-2 (PDB entry 3LN1).

Reference

1. Abbott, J. D.; Moreland, L. W. Expert Opin. Investig.Drugs2004, 13, 1007-1018.

2. Coulthard, L. G.; Costello, J.; Robinson, B.; Shiels, I. A.; Taylor, S. M.; Trent, M.;Woodruff,

T. M. Arthritis Res. Ther.2011, 13, R42.

3. Smith, W. L.; DeWitt, D. L.Adv. Immunol.1996, 62, 167-215..

4. Meade, E. A.; Smith, W. L.; DeWitt, D. L.J. Biol. Chem.1993,268, 6610-6614.

5. Brooks, P. M.; Day, R. O.N. Engl. J. Med. 1991, 324, 1716-1725.

6. Cathella-Lawson, F.; Reilly, M. P.; Kapoor, S. C. N. Engl. J. Med.2001, 345, 1809-1817.

7. Vane, J.; Botting, R. M. Am. J. Med. 1998, 104, S2-S8.

8. Rodriguez, L. A. Clin. Exp. Rheumatol. 2001, 19, S41-S44.

9. Patel, M. V.; Bell, R.; Majest, S.; Henry, R.; Kolasa, T.J.Org. Chem.2004,69, 7058-7065.

10. Brooking, P.; Doran,A.; Grimsey, P.; Hird, N. W.; MacLachlan, W. S.; Vimil,M.

Tetrahedron Lett. 1999, 40, 1405-1408.

PP-82

Design and Synthesis of 2-Pyridone Based Flexible Dimers and Their

Conformational Study through XRD and DFT: Perspective of Cyclooxygenase-

2 Inhibition1

Sunil K. Rai and Ashish K. Tewari*


264

Department of Chemistry (Center of Advanced Study), Faculty of Science, Banaras Hindu University,

Varanasi 221005, India.


This work describesthe results of X-ray crystallography of4-methyl-2-oxo-6-phenyl-1,2-

dihydropyridine-3-carbonitrile(1) and its propylene bridged dimers 2 and 3. Influence of inter and

intramolecular interactions on the conformation of propylene linker have been studied through

single crystal X-ray crystallography and DFT studies. Hirshfeld Surface analysishas been

employed for the study of intermolecular interactions. However, DSC analysis of compound 2 and

3, and TGA analysis of compound 3 has been performed to know the thermal stability. Along with

their molecular packing and thermal analysis, the molecular dockinghas also been performed in

the catalytic site of cyclooxygenase-2 to identify the potential anti-inflammatory activity of dimer

2 and 3. The above results suggest that the supramolecular aggregate structures which are formed

in solution are of lowest energy. However, cyclooxygenase-2 active site prefers the higher energy

conformers.

Figure 1.Docked pose of compound 2 (left) and within COX-2 (PDB entry 3LN1) and Hirshfeld

surface representation of 3 (right) showing C-H π interactions.

Reference:

S. K. Rai, S. Khanam, R. S. Khanna, A. K. Tewari, Cryst. Growth Des. 2015, DOI:

10.1021/cg501793v.

PP-83

Synthesis and Self Assembly of Tripodal Supramolecular Architecture

Archana Gaurav, Ranjeet Kumar, Ranjana S. Khanna and Ashish Kumar Tewari

Department of Chemistry, Faculty of Science, Banaras Hindu University, Varanasi



265


Feeble interactions between molecules play important role in various supramolecular

phenomena. Their investigation became the driving force for the development of

supramolecular chemistry. Intramolecular H-bonds are widely spread in organic compounds,

from common examples—such as the dimers of carboxylic acids, to the formation of large

aggregates such as capsules, supramolecular polymers and macrocycles. A number of

hydrogen-bonded aggregates have been obtained by self organization of organic or organic–

inorganic components. We herein report a bowl shaped box having fixed ring obtained by the

assembly of organic tripodal 2,2',2''-(((1,3,5-triazine-2,4,6-triyl)tris(sulfanediyl))tris(propane-

3,1-diyl))tris(3-oxo-5,6-diphenyl-2,3-dihydropyridazine-4-carbonitrile) as box and

chloroform as ring. This reaction is carried out from thiocynuric acid and 2-(3-bromopropyl)-

3-oxo-5,6-diphenyl-2,3-dihydropyridazine-4-carbonitrile at 800C in DMF. Given compound is

characterized by Single crystal x-ray analysis, 1H NMR and 2D NOSEY and AFM.

PP-84

Synthesis and antimicrobial evaluations of diarylchromene analogs

Parmesh K. Dwivedia, Devdutt Chaturvedia,*, Amit K. Chaturvedi2

aLaboratory of Medicinal Chemistry, Amity Institute of Pharmacy, Amity University Uttar Pradesh,

Lucknow Campus, Lucknow-226028, U. P.

bDepartment of Chemistry, G.L.A. University-281406, Mathura, U. P.



266

* Corresponding author’s e-mail: [email protected]

ABSTRACT

Chromenes are important class of compounds that have been used for fertility regulation. From

the plant Wisteria sinensis and Calyptranthes tricona, naturally occurring chromemnes have been

isolated. The chromene skeletons have also elicited pharmaceutical interest as structural elements

in drug-like compounds. Examples of artificial compounds bearing the 2H-chromene motif include

6-fluoro-2H-chromene, which exhibited the highest 5-HT1A receptor affinity among a series of

novel 6-fluorochromane derivatives; and 6-substituted 2H-chromenyl compound, which were

tested for potential antidiabetic activity. Structure activity relationship (SAR) studies with 3,4-

diaryl chromenes have suggested that p-position of the 4-phenyl residue as the most suitable place

for anchoring the basic chain. In the present study, the synthesis of carbamates derivatives of 3,4-

diarlychromenes of the following prototypes have been carried out and evaluated for antimicrobial

activities.

O

O

MeO

O C

O

N

R1

R2

n

Designed prototype

References:

1. Falkenstein, E.; Tillman, H.C.; Christ, M.; Feuring, M.; Wehling, M., (2000) Multiple actions

of steroid hormones--a focus on rapid, nongenomic effects, Pharmacological Review, 52, 513-

555.

2. Dardes, R.C.; Jordon, V.C., (2000) Novel agents to modulate oestrogen action, British Medical

Bulletin, 56, 773-786.

3. Hess, R.A.; Bunick, D.; Bahr, J., (2001) Oestrogen, its receptors and function in the male

reproductive tract - a review, Molecular and Cellular Endocrinology, 178, 29-38.

4. Glazier, M.G.; Bowman, M.A., (2001) A review of the evidence for the use of phytoestrogens

as a replacement for traditional estrogen replacement therapy, Arch. of Internal Medicine, 161,

1161-1172.

PP-85


267

Dithiocarbamate derivatives of zerumbone: A novel class of antimicrobial and

anticancer agents

Devdutt Chaturvedi, a,b*Parmesh K. Dwivedi,a,f Amit K. Chaturvedi,e Nisha Mishra,e Shagun Vaid,c

Madhunika Sharma,c Ajit K. Saxena,c Inshad A. Khan,d H. H. Siddiqui,f Virendra Mishrae

a Laboratory of Medicinal Chemistry, Amity Institute of Pharmacy, Amity University Uttar Pradesh,

Lucknow Campus, Lucknow-226028, U. P., India.

bBioorganic Chemistry Division, Indian Institute of Integrative Medicine (CSIR), Canal Road, Jammu-

Tawi-180001, J. & K., India.

c Cancer Pharmacology Division, Indian Institute of Integrative Medicine (CSIR), Canal Road, Jammu-

Tawi-180001, J. & K., India.

dClinical Microbiology Laboratory, Biotechnology Division, Indian Institute of Integrative Medicine

(CSIR), Canal Road, Jammu-Tawi-180001, J. & K., India.

e Synthetic Research Laboratory, B. S. A. P. G. College, Mathura-281004, U. P., India.

f Faculty of Pharmacy, Intergral University, Lucknow-, U. P. , India.

* Corresponding author. Tel.:91-522-2994778-82 Extn. 1052; E-mails: [email protected];

[email protected]

Abstract:

Natural products played important role in drug discovery research. Many of them have been

approved as drugs, prodrugs and drug candidates. Synthetic modifications of biologically active

natural products have been carried out to generate semisynthetic derivatives of natural products.

Several of semisynthetic analogs have been proved to become more potent drug candidate than

their parent molecules. In recent years, in order to search for more potent new drugs from the

biologically active natural products, synthetic modifications of natural products have become an

important tool to develop more potent drug like molecules.

Zerumbone, a monocyclic crystalline sesquiterpenoid containing cross-conjugated dienone

moiety reported by Sukh Devin 1960 from the major component of essential oil of the wild

gingerZingiber zerumbet Smith.1 The rhizomes of this plant are employed as traditional medicine

in relieving stomach ache, as a diuretic and when macerated in alcohol are regarded as a tonic and

depurative. Zerumbone and its derivatives have displayed a broad arrays of potential biological

activities such as anti-cancer,2 anti-inflammatory,3 antimicrobial (anti-bacterial,4& antifungal),




268

anti-cholinesterase, anti-HIV,5antinociceptive, and hepatoprotective etc. Furthermore, zerumbone

exhibits anti-proliferative and anti-inflammatory activities but underlying molecular mechanisms

are poorly understood. In the present paper, a novel series of β-substituted ethyl dithiocarbamates

derivatives of zerumbone has been synthesized employing Michael addition approach and their

anti-microbial and anti-cancer activities were evaluated. Some of these compounds have shown

promising antimicrobial and anticancer activities. The details of research work carried out will be

presented.

PP-86

Entinostat — a ray of hope in breast cancer

Pragyandip P. Dash,a Devdutt Chaturvedi,,a and Anuradha Mishrab

aLaboratory of Medicinal Chemistry, Amity Institute of Pharmacy, Amity University Uttar

Pradesh, Lucknow Campus, Lucknow-226028, U. P., India.

bFaculty of Pharmacy, Integral University, Lucknow-226026, U. P. , India

ABSTRACT

Entinostat, also known as SNDX-275 and MS-275, is a benzamidehistone deacetylase inhibitor

undergoing clinical trials for treatment of various cancers. Entinostat inhibits class I HDAC1 and

HDAC3 with IC50 of 0.51 μM and 1.7 μM, respectively.Syndax’s lead product entinostat has been

studied in more than 600 cancer patients where objective tumor responses have been observed in both

solid and hematologic malignancies. Entinostat’s established safety profile as both a single agent and

in combination with a number of commercially available targeted therapies differentiates it from other

histone deacetylase (HDAC) inhibitors. Having shown potential in breast and lung cancer, entinostat

is moving toward pivotal clinical testing. It is a novel inhibitor of class I histone deacetylases, key

enzymes that alter the structure of chromatin to control gene expression. This aberrant gene expression

can result in reversible, epigenetically-based drug tolerance. Designed to selectively target the HDAC

isoforms most relevant to the biology of tumors, entinostat can normalize dysregulated gene

expression in cancer cells.

PP-87

Evaluation of anti-inflammatory activity of methanolic extract of Haldina

cordifolia

P. P. Dash1*, A. Mishra 2 and S.R.Swain3

1Amity Institute of Pharmacy, Amity University Lucknow.

http://en.wikipedia.org/wiki/Benzamide

http://en.wikipedia.org/wiki/Benzamide

http://en.wikipedia.org/wiki/HDAC1

http://en.wikipedia.org/wiki/HDAC3

http://en.wikipedia.org/wiki/IC50


269

2 Faculty of Pharmacy, Integral University Lucknow.

3Sherwood college of Pharmacy, Barabanki.

ABSTRACT

Herbalism or "herbal medicines" have a long history to cure several kinds of human diseases from the

various parts of the plants such as leaf, stem, bark, root, etc.2 Plants have been the basis for medical

treatments through much of human history, and such traditional medicine is still widely practiced

today. Modern medicine recognizes herbalism as a form of alternative medicine, as the practice of

herbalism is not strictly based on evidence gathered using the scientific method.Many of the

pharmaceuticals currently available to physicians have a long history of use as herbal remedies,

including opium, aspirin, digitalis, and quinine. The World Health Organization (WHO) estimates that

80 percent of the population of some Asian and African countries presently uses.herbal medicines for

some aspect of primary health care.Haldina cordifolia had been extensively used for its reported

biological action in indigenous organization of medicine. The at hand investigation was carried out

to discover the anti-inflammatory effect of methanolic extract of Haldina cordifolia in albino rats. The

anti-inflammatory activity was evaluated by means of acute inflammatory model like carrageenan

induced paw edema and chronic inflammatory model like cotton pellet induced granuloma

respectively. The methanolic extract in different doses (100,200, and 400mg/kg, p .o) exhibited

dose dependent and significant anti-inflammatory activity in acute (carageenan induced hind

paw edema, p<0.05) and chronic (cotton pellet granuloma formation, p<0.05) model of

inflammation.

PP-88

Synthesis of Primaquine Glyco-conjugates at physiological pH as potential

tissue-schizontocidal antimalarial agents

Mridula Saxena,*,a Chandra S. Azadb and Anil. K. Saxenab

aDepartment of Appled Chemistry, Amity School of Applied Sciences, Amity University Uttar Pradesh,

Lucknow Campus, Lucknow-226028, U. P., India

b. Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow-226028, U. P.,

India.

Tel.: (+91-522) 400-42-80, e-mail: [email protected]

ABSTRACT

Malaria is a parasitic disease affecting nearly 200 million persons across the globe and led to 627

thousands deaths in 2012. The most currently used antimalarials are potent blood schizontocidals;

i.e., they act rapidly against the parasite forms that invade erythrocytes and cause the well-

described malaria symptoms. Among the plethora of antimalarial drugs, 8-aminoquinolines are the

http://en.wikipedia.org/wiki/Traditional_medicine

http://en.wikipedia.org/wiki/Alternative_medicine

http://en.wikipedia.org/wiki/Evidence

http://en.wikipedia.org/wiki/Scientific_method

http://en.wikipedia.org/wiki/Pharmaceuticals

http://en.wikipedia.org/wiki/Opium

http://en.wikipedia.org/wiki/Aspirin

http://en.wikipedia.org/wiki/Digitalis

http://en.wikipedia.org/wiki/Quinine

http://en.wikipedia.org/wiki/World_Health_Organization


270

most potent class of malarial drugs with radical curative activity, having properties to eliminate

the hypnozoites from the liver. Among the important 8-aminoquinoline derivatives Primaquine

(PQ) is the most effective being the only drug available for tissue schizonticidal activity in P.vivax

malaria and gametocidal activity in P. falciparum infection. It is the toxicity of the PQ which limits

its clinical utility in therapeutic applications. The most serious side effect of the PQ is the

haemolysis particularly in individuals with heredity deficiency of G6PD (glucose-6-phophate

dehydrogenase). The other significant side effect associated with PQ and 8-aminoquinoline

derivatives are methemoglobinemia, leucopoenia, abdominal cramps, and epigestric distress. To

overcome these side effects we tried to synthesised the N-Glycoconjugates of Primaquine based

on the hypothesis that receptor on plasma membrane of liver parenchymal cells and liver von

kupffer cells recognize hexose like galactose and mannose respectively. From this it would appear

that the title compound with hexopyranose part as galactose or mannose may direct the primaquine

to the liver where the latent tissue forms exist. This may result in substantial decrease in its

systemic circulation which may reduce the hematological toxicity and increase in its selectivity.

The reactivity of the hexoses towards PQ in yielding the PQ-glyco-conjugate may depend on the

stereochemistry and reactivity of the hexoses. This may influence the formation of mixture of α/β

epimers. Thus optimization of the N-glycosylation reaction in terms of yield, reaction time, and

diastereoselectivity was a significant challenge. Several attempts were made for the synthesis of

glyco-conjugate e.g. condensing the halide donor of hexose with PQ base or PQ diphosphate in

DCM/acetone/DMF using variety of bases, but non-separable mixture was obtained. The photo-

sesitivity of PQ was also taken in to the account and all the reactions were performed in dark. It is

well recognized that the reaction between an amine and reducible sugar such as D-glucose in water,

at high temperature and in slightly low pH first proceeds through the unstable corresponding N-

glycoside, which undergoes the Amadori rearrangement to produce the Amadori product. When

the reaction of PQ-base and D glucose in C2H5OH was carried out a new compound containing

hexose and PQ was formed (yield 50%), this led to the selection of EtOH as a solvent of choice

for the model reaction. The formation of the compound containing both PQ and D-glucose was

confirmed by the UV absorption and charring test for the hexose counterpart. Its 1H NMR analysis

revealed that product was not the N-glycoside, because there was no signal of anomeric proton in

the expected region (range 4.5- 6.2 ppm) and instead there were two double multiplets at 4.04-4.26

ppm and at 2.66-3.02 ppm of CH2 thus indicative of the formation of Amadori products. This was

further confirmed by the reported spectra corresponding to Amadori products and 13C NMR. So

we focused on the normal glycosylation process occurred in body and thought that at physiological

pH compound should be formed. Hence we tried the reaction of PQ base and hexose in phosphate

buffer and we got single N-glycoside as expected. The pH as well as reaction temperature were

further optimized to get single isomer of N-glycosylated PQ. All the natural available hexoses

were used in the study and we successfully synthesised the and isomers of the corresponding

hexoses. The preference for formation of the isomer in some compunds over can be

rationalized in terms of the competition between substitution at the sterically least hindered


271

position () against the substitution at a position which sustains stabilization from the anomeric

effect (). The substitution is driven predominantly by the steric factor thus the reaction is found

stereoselective for the configuration.

The antimalarial activitiy of hexose (galactoside/glucoside) conjugated Primaquine was better than

the activities of PQ. To conclude, the prominent in vivo efficacy of the galactoside conjugate over

premaquin (PQ) in cyanomolgi infected rhesus monkey is indicative of the potential utility of these

compounds in the therapy of malaria infection caused by P. vivox.

PP-89

A new triterpene from the leaves of Ceriops tagel

Devdutt Chaturvedia,* Rajesh Kumar,bAmit K. Chaturvedi,c

aLaboratory of Medicinal Chemistry, Amity Institute of Pharmacy,Amity University Uttar Pradesh

(AUUP), Lucknow Campus, Lucknow-226028, U.P., India

bChemical Research Division, Ranbaxy Research Laboratories Ltd., Gurgaon-122001, Haryana, India.

cDepartment of Chemistry, GLA-University, Mathura-281406, U. P., India

*Corresponding author’s e-mails: [email protected]

ABSTRACT

Ceriops tagel (Perr.) (Family: Rhizophoraceae) is a mangrove shrub, found along the coastal

forests of peninsular India, in the Sundar bans of West Bengal and Andaman and Nicobar Islands.

Mangrove plants of genus Ceriops represented by two species, C. decandra and C. tagel are widely

distributed along the sea coasts of Africa, South Asia, and South Pacific islands [1]. These plants

are used as a folk remedy e.g. against sores [2]. The plant possesses astringent properties; the

decoction of the bark is used to stop hemorrhage and is applied to malignant ulcers [3]. Shoot is

used as a substitute for quinine in Africa [4]. The boiled fruits are eaten in Andaman [5]. A

literature survey of this plant revealed that seven dolabrane-type diterpenes namely tagalsins A-G

and one norditerpenewere isolated from the stem and twigs [6]. Five dammaranetriterpenes,

oleanolic acid, 3β-E-feruloyllupeol, 3β-Z-feruloyllupeol, 3β-E-feruloyl-betulin, 3β-E-

feruloylbetulinic acid, 3β-E-caffeoylbetulinic acid, 3β-E-caffeoylbetulin, 3β-E-coumaroyllupeol,

3β-E-acetylbetulinic acid, betulin, betulinic acid, 3α-betulinic acid, betulonic acid and lupeol were

isolated from the hypocotyls and fruits of Ceriopstagel [7]. The present communication deals with

the isolation and characterisation of novel triterpene from the leaves of plant designated as p-acetyl

coumaryl ester of lupeol (Fig.1).



272

O

3

1

29

30

28

19

O

O

O 1'

4'

7'

Figure 1. Chemical structure of p-acetyl coumaryl ester of lupeol

References:

[1] A. S. R. Anjaneyulu and V. L. Rao, Phytochemistry,2002,60, 777.

[2] P. Lin and Q. Fu, Environmental ecology and economic utilization of mangroves

in China, Higher education press, Beijing, 1995.

[3] R. P. Rastogi and B. N. Mehrotra, Compendium of Indian medicinal plants vol.

1, Publications and Information Directorate, New Delhi, 1991.

[4] K. R. Kartikar and B. D. Basu and an I. C. S. (rtd); revised by E. Blatter, J. F.

Caius and K. S. Mhaskar (LalitMohan Basu, Allahabad), Indian Medicinal

Plants, 2nd.edn, 4 Vols, 1935.

[5] Sangal Indian For, 1971, 97, 646.

[6] Y. Zang, Z. Deng, T. Gao, P. Proksch, W. Lin, Phytochemistry,2005, 66, 1465.

[7] C. Pakhathirathien, C. Karalai, C. Ponglimanont, S. Subhadhirasakul and K.

Chantrapromma, J. Nat. Prod., 2005,68, 1787.

PP-90

Formulation & Evaluation of Chronomodulated drug delivery system of an

Anti –inflammatory drug Sarita Pal, Nimisha

Amity Institute of Pharmacy, Amity University Uttar Pradesh, Lucknow Campus.

ABSTRACT

Drug delivery systems with a pulsatile release pattern are growingon increase in the interest for the

development of drugs, where conventional drug release systems are not ideal. A pulse has to be


273

designed in such a way that a complete and rapid drug release is achieved after the lag time so as to

match body’s circadian rhythms, with the release of drug which increases the efficacy and safety of

drugs by proportioning their peak plasma concentrations during the 24 hours in synchrony with

biological rhythm. These systems are beneficial for those drugs which exhibited

chronopharmacological behavior as well as for those drugs having high first pass metabolism,where

night time dosing is required. In the present study, we have developed a novel drug delivery system

by implementing chronopharmaceutical approach for the treatment of arthritis, using Tapentadol

hydrochloride drug. Tapentadol is a drug of NSAIDs category, which are used to relieve pain and

inflammation associated with arthritis and its related conditions. The half-life of Tapentadol is about

4 hours and oral dose is 50 to 250 mg twice a day. In this study we have formulated Tapentadol tablet

by direct compression method using Ethyl cellulose as a polymer and coated with Eudragit S100, lag

time of 5.5 hrs with cumulative drug release of 98% within 10 hrs.

PP-91

Pharmacological and Bio-Molecular Investigation of Curcumin for Anti-

asthmatic Activity

Sarkar Saikat, Sajal Srivastava, Parmesh Kr Dwivedi, Rahul Shukla

The efficiency of ethanolic extract of Curcuma longain reverting deviated bio-molecular parameters

in asthma were assessed in the study by evaluating Myeloperoxidase, Malonyldialdehyde, Nitric

oxide, Blood urea nitrogen, Lung alveolar lavage, Hematological aberrations, Histopathological

changes in spague dawley rats for a duration of 30 days (Short term) and 120 days (Long term).

Asthma was induced in the animals by egg white solution supplemented with aluminium hydroxide

and the animals were categorized into five groups, one group was not induced asthma and not treated,

another group was asthma induced and was left untreated, another asthma induced group received

standard drug and two groups received investigated extract in doses of 300 and 500 mg respectively

to study dose response of the extract.

PP-92

DESIGN OF SOME NOVEL AROMATIC AMIDES AGAINST

AEDES AEGYPTI MOSQUITOES

Akanksha Garud

School of Studies in Pharmaceutical Sciences, Jiwaji University, Gwalior (M.P.)

Introduction: In the history of the world, more people have died from diseases transmitted by

mosquitoes than from all the fighting in all the wars. Over two billion people in tropical countries,


274

like India, are at risk. Globally, Malaria kills about 3 million each year, including 1 child every 30

seconds.

Aims and Objective: Keeping this in view, a series of substituted aromatic amides by varying the

chain length, substitution of methyl, methoxy, chloro, and fuoro groups at ortho-, meta-, and para-

positions of the phenyl ring of N,N-diethyl-2-phenylacetamide were synthesized.

Methodology: Laboratory studies were carried out to observe the behavioral responses and

repellent activity of these newly synthesized aromatic amides against Aedes aegypti mosquitoes..

Results: These aromatic amides were tested for their behavioral responses and compared with the

well known insect repellents, namely, N,N-diethyl toluamide; N,N-diethyl phenylacetamide; and

N,N-diethylbenzamide. Out of the 14 compounds synthesized, seven compounds were selected on

the basis of those showing 75% of repellent response for the bioefficacy test on human volunteers.

Conclusion: In lack of effective vaccine, personal protection management is the need of todayand

is apparently practicaland economical alternative to insecticides.

Keywords: mosquito, repellent, amide, behavioral response, Aedes aegypti

References:

Kumar, S., S. Prakash, R. K. Sharma, S. K. Jain, M. Kalyanasundaram, R. V. Swamy, and K. M.

Rao. 1984. Field evaluation of three repellents against mosquitoes, black fies and land leeches.

Indian J. Med. Res. 80: 541.

Ma, D., A. K. Bhattacharjee, R. K. Gupta, and J. M. Karle. 1999. Predicting mosquito repellent

potency of N,N-diethyl-m-toluamide (DEET) analogs from molecular electronic properties. Am.

J. Trop. Med. Hyg. 60: 1-6.

PP-93

TREATMENT OF LIFESTYLE DISORDERS BY HERBAL MEDICATION

Priyanka Srivastava, Alka Rai, Mini Singh, Richa Srivastava

Amity Institute of Pharmacy, Lucknow Campus.

ABSTRACT

As the elderly population grows, so does the incidence of cardiovascular disease and the use of

medications. Because of the side effects and cost of prescribed medicine, many aging individuals

are seeking out alternative treatment options. Complementary and alternative medicine is gaining

popularity, with about a third of people older than 60 years currently using one or more of these


275

therapies. Many individuals are using herbs and nutritional supplements to prevent and treat a

variety of cardiovascular diseases and their symptoms. Herbs and nutritional supplements are

considered food by the Food and Drug Administration and are exempt from mandatory testing for

their safety or efficacy. Also, many individuals consider these products as natural and do not

recognize the negative impact that these alternative treatments may have on the efficacy of

prescribed medications and overall health. Part of the problem for both consumers and physicians

has been the paucity of scientific data on herbal medicines. As a result, those who wish to obtain

factual information regarding the therapeutic use or potential harm of herbal remedies would have

to obtain it from books and pamphlets, most of which base their information on traditional

reputation rather than relying on existing scientific research. One may wonder why the herbal

industry never chose to simply prove its products safe and effective. The answer is primarily

economical. With the slim chance of patent protection for the many herbs that have been in use for

centuries, pharmaceutical companies have not provided financial support for research on the merits

of herbal medicine. To date, research has reported conflicting evidence as to the beneficial effects

of these products; health care providers should exercise caution in recommending their use to avoid

drug interactions and side effects.

PP-94

SYNTHESIS OF BENZENEPROPANAMINE ANALOGUES AS POSSIBLE

SPERMICIDES

Anjali Mishra, Suyash Tiwari, Vishnu Lal Sharma

Medicinal and Process Chemistry Division

CSIR-Central Drug Research Institute,Lucknow, 226031 (INDIA)

ABSTRACT

The current worldwide population is expected to increase by more than 50% by the year 2050.

This is likely to be accompanied by an equally challenging rise in number of STV and HIV

infections. Dually active, prophylactic vaginal contraceptives can effectively tackle these

problems. Specific sulfhydryl alkylating agents like N-alkylmaleimide derivatives possesses

spermicidal activity. Moreover paroxetine, arylmethylaryl piperidine and fluoxetine, an

aryloxyphenylpropylamine which interact with sulfhydryl groups have been recently reported to

possess spermicidal activities. These observations prompted us to synthesize some

benzenepropanamine analogues (fig.1) with various groups at aryl-alkyl junction (X) and with

substituted amine residues of increasing ring size (NR1R2) and to evaluate for spermicidal activity.


276

XN

R1

R2

NR2

R1=

NN N

X =

O OH

O

CF3

Fig 1: General Structure of Synthesized Compounds

Keywords: spermicidal, benzenepropanamine.

Ref: Kumar, K.; Sharma, V.L; Kumar, M.; Shukla, K.P; Tiwari, P.; Jain, R.K.; Maikhuri, J.P.;

Singh, D.; Gupta, G.; Singh, M.M. Bioorg. Med. Chem. 2006, 14, 6593-6600.

PP-95

SYNTHESIS OF 1-DIALKYLAMINOCARBOTHIOIC ACID S-[(2,3

EPITHIO)PROPYL] ESTER AND DERIVATIVES HAVING

SPERMICIDAL ACTIVITY

Suyash Tiwari, Anjali Mishra, Vishnu Lal Sharma

Medicinal and Process Chemistry Division, CSIR-CDRI

Lucknow, 226031(INDIA)

ABSTRACT

Dialkyl-amino carbothioic acid esters are valuable class of intermediate leading to compound

having spermicidal activity. These types of compounds also find their use as additives for synthetic

and natural lubricants.

A simple and convenient method for the synthesis of 1-dialkyl amino carbothioic acid S-[(2,3-

epithio)propyl]ester is being developed by the reaction of 1-dialkylaminocarbodithioic acid-

sodium salt with epichlorohydrin in water-methanol mixture at room temperature. This

intermediate will be further subjected to its use in the synthesis of spermicidal agents.


277

KEY WORDS:Dialkyl-amino carbothioic acid,spermicide,epichlorohydrin.

REFERENCE:

Kumar, K.; Sharma, V. L.; Dwivedi, A. K. J. Heterocyclic. Chem. 43, 1 (2006).

PP-96

TREATMENT OF LIFESTYLE DISORDERS BY HERBAL MEDICATION

Priyanka Srivastava, Alka Rai, Mini Singh, Richa Srivastava

Amity Institute of Pharmacy, Lucknow Campus.

ABSTRACT

As the elderly population grows, so does the incidence of cardiovascular disease and the use of

medications. Because of the side effects and cost of prescribed medicine, many aging individuals

are seeking out alternative treatment options. Complementary and alternative medicine is gaining

popularity, with about a third of people older than 60 years currently using one or more of these

therapies. Many individuals are using herbs and nutritional supplements to prevent and treat a

variety of cardiovascular diseases and their symptoms. Herbs and nutritional supplements are

considered food by the Food and Drug Administration and are exempt from mandatory testing for

their safety or efficacy. Also, many individuals consider these products as natural and do not

recognize the negative impact that these alternative treatments may have on the efficacy of

prescribed medications and overall health. Part of the problem for both consumers and physicians

has been the paucity of scientific data on herbal medicines. As a result, those who wish to obtain

factual information regarding the therapeutic use or potential harm of herbal remedies would have

to obtain it from books and pamphlets, most of which base their information on traditional

reputation rather than relying on existing scientific research. One may wonder why the herbal

industry never chose to simply prove its products safe and effective. The answer is primarily

economical. With the slim chance of patent protection for the many herbs that have been in use for

centuries, pharmaceutical companies have not provided financial support for research on the merits

of herbal medicine. To date, research has reported conflicting evidence as to the beneficial effects

of these products; health care providers should exercise caution in recommending their use to avoid

drug interactions and side effects.


278

PP-97

Stereoselective total synthesis of cytotoxic oxylipin Topsentolide B2

Devdutt Chaturvedi,a,* Amit K. Chaturvedi,b Sadaf Zaidi,a




ABSTRACT

Marine metabolites containing a trans-disubstituted cyclopropane subunit and saturated

and unsaturated lactones of various ring sizes, which are called oxylipins, are a growing class of

natural products.1 Topsentolide is an oxylipin isolated from the methanol extract of a marine

sponge Topsentia sp along with six other metabolites. This nine membered lactone possess

moderate cytotoxicity against a panel of human solid tumor cell lines. To best of our knowledge,

no total synthesis of this molecule is reported till date. In the present paper, we have reported an

efficient stereoselective synthesis of marine oxylipin Topsentolide B2 1 is described. The key steps

involved are Yamaguchi coupling, ring closing metathesis and Julia-Kocienski olefination

(Scheme 1).

.

HO OH

OOOO

S

O

ON N

NN

Ph

HO

OP

OP

PO

O

OP

1 2 3

4 5

Scheme 1

PP-98


279

CHARACTERIZATION OF MACROCYCLIC COMPLEXES

SYNTHESIZED BY SONOCHEMICAL METHOD: A GREEN APPROACH Dr Monika Kamboj

Asst Prof III

Department of Chemistry,

Amity School of Applied Sciences



ABSTRACT

Macrocyclic ligands and their metal complexes is a growing area of research in inorganic and

bioinorganic chemistry in view of their presence in many biologically significant systems. The

metal complexes containing synthetic macrocyclic ligands have attracted a great deal of attention

because they can be used as models for more intricate biological macrocyclic systems:

metalloporpyrins (hemoglobin, myoglobin, cytochromes and chlorophylls), corrins (vitamin B12)

and antibiotics (valinomycin, nonactin). The possibility of using synthetic macrocycles as models

for the biological systems has provided an impetus for much of this research.

Synthesis of macrocyclic complexes by Sonochemical method is new synthetic technique,

a green approach. Ultrasound is the name given to sound waves having frequencies higher than

those to which human ears can respond, i.e. greater than 16kHz and with wavelength between 7.0

and 0.015 cm. It is transmitted through any substance-solid, liquid or gas, which possesses elastic

properties. Ultrasound provides an unusual mechanism for generating high-energy chemistry

which extremely high local temperatures and pressures and an extraordinary heating and cooling

rate. Initially, the use of ultrasound was restricted. However, it has increased manifold in a variety

of chemical reactions, resulting in a sub-discipline called ‘Sonochemistry’.Sonochemistry derives

principally from acoustic cavitation: the formation, growth, and implosive collapse of bubbles in

liquids. Cavitation serves as a means of concentrating the diffuse energy of sound. Transition metal

Macrocyclic complexes synthesized by Template method under ultrasonic irradiation and their

characterization are discussed in this paper.

Keywords: Macrocyclic, Sonochemistry, acoustic cavitation, Template method

ACKNOWLEDGEMENTS

We are grateful to our Chancellor, Vice-Chancellor, Pro-Vice Chancellor, Amity University,

Lucknow Campus, for encouraging and supporting the National Symposium ICBDD, 2015. We

are also grateful to Prof. Dr. W. Selvamurthy, President, Science & Technology, Amity University,

Prof. Dr. Q. Rahman, Dean and Director Research (Science and Technology), Prof. Dr. M. V.

Ramana, Director, AIP for encouraging and proper guidance for the grand success of the


280

symposium. We are grateful to Dr. Nitya Anand, Former Director, CSIR-Central Drug Research

Institute (CDRI), for his kind acceptance as a Chief Guest and for giving his very excellent and

illuminating talk on “Interfacing Chemical Biology and Pharmaceutical Practices.” We are also

grateful to all our eminent invited speakers from different the academic institutions mainly Prof.

P. Pramanik (IIT, Kharagpur), Dr. Anil K. Saxena (CSIR-CDRI, Lucknow), Prof. Vishnu K.

Tandon ( University of Lucknow), Prof. Rahul Jain (NIPER, Mohali), Dr. Rakesh Maurya (CSIR-

CDRI, Lucknow), Dr. H. M. Sampath Kumar (CSIR-IICT, Hyderabad), Dr. Arvind S. Negi (CSIR-

CIMAP, Lucknow), Prof. G. Brahmachari ( Visva-Bharati, Santiniketan, a Central University,

West Bengal), Dr. Anil K. Dwivedi (CSIR-CDRI, Lucknow), Dr. Ajit K. Saxena ( Amity

University, Lucknow Campus), Dr. A. K. S. Rawat (CSIR-NBRI, Lucknow), Dr. Javed Ali (Jamia

Hamdard University, New Delhi), Dr. Atul Kumar (CSIR-CDRI), Dr. R. P. Tripathi (CSIR-CDRI,

Lucknow), Dr. Ram A. Vishwakarma (CSIR-IIIM, Jammu), Dr. Vinod K. Tiwari (BHU,

Varanasi), and Dr. Ram Sagar Misra (Shiv Nadar University, Noida) etc. We are also thankful to

all the delegates from the all parts of India for making the grand success of the symposium.

We are thankful to Department of Science and Technology (DST), Govt. of India,

New Delhi, and India Council of Medical Research (ICMR), New Delhi, for financial support of

the symposium.

We are grateful to Prof. Goutam Brahmachari, Editor-in Chief of the journal and Dr. S.

Pandalai, Publisher, SOA Journal of Organic and Biomolecular Chemistry, for his keen interest

and carry forward in publishing this ICBDD, 2015 symposium issue.

Some Photographs of the National Symposium on Interfacing Chemical Biology and Drug

Design (ICBDD), 24-25th Feb. 2015


281


282

Group of Senior Invitees along with Hon. Pro-V. C. releasing the Abstract Book of ICBDD,


283

Prof. Dr. Q. Rahman, Dean & Director Research, Science and Technology, Addressing the

gathering


284

Dr. M. V. Ramana, Director, AIP, addressing the gathering

Dr. Nitya Anand, The Chief Guest, delivering his talk

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