Synthesis, antiplatelet activity and comparative molecular field analysis of substituted 2-amino-4H-pyrido [1, 2-a] pyrimidin-4-ones, their congeners and isosteric …

…, N Cinone, M Di Braccio, G Grossi, G Leoncini…

Index: Roma, Giorgio; Cinone, Nunzia; Di Braccio, Mario; Grossi, Giancarlo; Leoncini, Giuliana; Signorello, Maria Grazia; Carotti, Angelo Bioorganic and Medicinal Chemistry, 2000 , vol. 8, # 4 p. 751 - 768

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Citation Number: 38

Abstract

2-(1-Piperazinyl)-4H-pyrido [1, 2-a] pyrimidin-4-one (5a) is a recently described in vitro inhibitor of human platelet aggregation which specifically inhibits the activity of high affinity cAMP phosphodiesterase. A number of substitution derivatives, isosteres, and analogues of 5a were now synthesized and tested in vitro for their inhibitory activity on human platelet aggregation induced in platelet-rich plasma by ADP, collagen, or the Ca2+ ionophore ...