Roma G, Di Braccio M, Leoncini G, Aprile B
Istituto di Scienze Farmaceutiche, Università di Genova, Italy.
Farmaco. 1993 Sep;48(9):1225-38.
The N-substituted 2-amino-4H-pyrido[1,2-a]pyrimidin-4-ones 2 d,g-i,l-p,r,s and derivatives 4,5 b,6 a,b, 7 a,b were prepared. Both these novel compounds (except the insoluble 7a) and compounds 2 a-c,e,f,j,k,q, 5a, previously prepared by us, were tested in vitro for their inhibitory activity on human platelet aggregation induced by ADP, collagen, or A23187. On the whole, the compounds tested proved to be more active towards collagen than towards ADP and A23187. The 2-(4-methyl-1-piperazinyl)derivative 2 g was the most active compound both towards ADP and collagen, whereas the 2-(diethylamino)derivative 2 b proved to be the most active one towards A23187.
制备了N-取代的2-氨基-4H-吡啶并[1,2-a]嘧啶-4-酮2 d、g-i、l-p、r、s以及衍生物4、5 b、6 a、b、7 a、b。我们之前制备的这些新型化合物（不包括不溶性的7a）以及化合物2 a-c、e、f、j、k、q、5a，均在体外测试了它们对由ADP、胶原或A23187诱导的人血小板聚集的抑制活性。总体而言，测试的化合物对胶原的活性比对ADP和A23187的活性更高。2-(4-甲基-1-哌嗪基)衍生物2 g是对ADP和胶原最具活性的化合物，而2-(二乙氨基)衍生物2 b被证明是对A23187最具活性的化合物。
