1,2-fused pyrimidines. VI. Substituted 2-amino-4H-pyrido[1,2-a]pyrimidin-4-ones with antiplatelet activity.
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.
Roma
G
G
Istituto di Scienze Farmaceutiche, Università di Genova, Italy.
Di Braccio
M
M
Leoncini
G
G
Aprile
B
B
D000244:Adenosine Diphosphate; D000001:Calcimycin; D003094:Collagen; D006801:Humans; D066298:In Vitro Techniques; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D011744:Pyrimidinones / Q000737:chemistry* / Q000494:pharmacology*
D010975:Platelet Aggregation Inhibitors; D011744:Pyrimidinones; D000001:Calcimycin; D000244:Adenosine Diphosphate; D003094:Collagen