[Synthesis and platelet aggregation inhibitory activity of 6-substituted dihydropyridazinones].
In order to develop more potent and less toxic antithrombotic agents, ten 6-(4-substituted piperazinyl acetyl aminophenyl)-4,5-dihydro-3(2H)-pyridazinones were synthesized. The title compounds were tested in vitro for platelet aggregation inhibitory activity with ADP-induced rat platelets and PAF-induced rabbit platelets. Preliminary tests showed that all of the pyridazinones could inhibit ADP-induced rat platelet aggregation. I7, I8, I9 were more potent than the control compound CI 930. I9 was the most potent compound with IC50 of 0.99 mumol/L. Pertaining to PAF-induced rabbit platelet aggregation, I9 was the most potent inhibitor with IC50 of 3.7 mumol/L.
Yao
F M
FM
Department of Pharmacy, Bethune International Peace Hospital, Shijiazhuang.
Sun
C S
CS
D000818:Animals; D010974:Platelet Aggregation / Q000187:drug effects; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011724:Pyridazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011817:Rabbits; D051381:Rats
D010975:Platelet Aggregation Inhibitors; D011724:Pyridazines