2001 pyrazine derivatives

pyrazine derivativesR 0550

03 - 136Synthesis, 5-HT1A and 5-HT2A Receptor Affinity of New 1-Phenylpiperazinylpropyl Derivatives of Purine-2,6- and Pyrrolidine-2,5-diones. — With the aim to evaluate the influence of the 1,3-diazepinering in compound (I) and of the spiroalkyl ring in (II) on their bindingaffinity and selectivity as 5-HT1A and 5-HT2A receptors, two series of1-phenylpiperazinylpropyl derivatives related to (I) and (II) are preparedand evaluated for their binding properties. It is shown that the structuralmodifications, i.e diazepine ring opening [cf. (V), (VII)] and replacement ofthe spiroalkyl moiety [cf. (IX), (XII)], do not improve binding affinity andselectivity. — (PAWLOWSKI, MACIEJ; CHLON, GRAZYNA; OBNISKA,JOLANTA; ZEJC, ALFRED; CHARAKCHIEVA-MINOL, SIJKA; MOKROSZ,MARIA J.; Farmaco 55 (2000) 6-7, 461-468; Dep. Pharm. Chem., Coll. Med.,Jagiellonian Univ., PL-30-688 Krakow, Pol.; EN)

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