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8/3/2019 Science Presentation-Analgesic Effect New Synthetic Drugs
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1/25/2012 1
ANALGESIC EFFECT OF NEW
SYNTHETIC DRUG BENZOFURAN-3,4-DIHYDROXY CHALCONE BY
HOT PLATE TESTS IN MICE
Theresia Ayu. Rayon 2443009070Edwin Jeika B. 2443009108
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OUTLINE
Introduction
Materials Methods
Results & Disscusion
Conclusions
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INTRODUCTION
Analgesic drugs relief pain
??
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Effiicacy &Unwanted
Effect
Need new
better drugs
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INTRODUCTION
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ChalconeDerivates
Anti-inflammatory effect andcancer chemo preventiveactivity
Hydroxy chalcones inhibit 12-lipoxygenase & cycloxygenase
Benzofuran-3-one Derivates
Anti-inflammatory effectRapidly and extensivelymetabolized after systemicadministration nontoxic
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INTRODUCTION : Purpose
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ChalconeDerivates
DerivatBenzofuran-3-one
Activity Tests
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MATERIALs
Synthesis
Pharmacology
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5-MethoxybenzofuranOxalyl ChlorideDiazomethane
Acetic Acid3,4-DihydroxybenzaldehydeDry HCl
Mice: Male SwissAlbino
with good housing
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METHODs
Synthesis ofDrugs:
Reaction &Crystalilzed
Pharmacology:
Analgesic Effecttested by Hotplate method
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O
O
O
Cl
2,5-dimethoxybenzoyl chloride
N+
N-
diazomethan
O
O
O
N N
2-diazo-1-(2,5-dimethoxyphenyl)ethanone
O
O
O
OH
2,5-dimethoxybenzoic acid
O
O
Cl
Cl
oxalyl dichloride
O
O
O
Cl
2,5-dimethoxybenzoyl chloride
Step 1
Step 2
Method: Synthesis
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O
O
O
N N
2-diazo-1-(2,5-dimethoxyphenyl)ethanone
O
OH
acetic acid
O
O
O
5-methoxybenzofuran-3(2H)-one
O
O
O
5-methoxybenzof uran-3(2H)-one
O
OH
OH
3,4-dihydroxybenzaldehyde O
O
OOH
OH
(z)-2-(3,4-dihydroxybenzylidene)-5-methoxybenzofuran-3(2h)-one
Step 3
Step 4
Method: Synthesis
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Benzofuran-3,4-dihydroxy
chalcone (BF-DK)
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Method : Hot Plate
Temperature 551C
Observation
0, 15, 30, 45, and 60 min after i.p.
lick the fore or hind paw or jump out
Quantitatif Maximum Possible Effect
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Method : Hot Plate
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Group 1 2 3 -controll +controll
Drug BF-
DK
BF-
DK
BF-
DK
Saline Morphin
e
Ibuprofen
Doses(mg/kg)
12,5 25 50 10ml/kg 2,5 200
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RESULT & DISCUSSION
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RESULT & DISSCUSION
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RESULT & DISSCUSION
Concentration of BF-DK, reached to max in
45 minutes after injection Metabolized
In acute phase, BF-DK equal to ibuprofen Analgesic effect of Benzofuran-3,4-dihydroxy
chalcone is lower than Morphine (central
analgesic)
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CONCLUSION
Drug have analgesic effect
Further research can be developing to
investigation the analgesic mechanisms ofthe drug
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