摘要
根据哒嗪酮类化合物的构效关系和作用机制 ,以CCI 17810为先导化合物 ,设计合成了 6 〔4 (取代哌嗪基 )苯基〕 5 甲基 4,5 二氢 3(2H)哒嗪酮类化合物 12个 .初步的体外药理试验表明 :大部分目标化合物都有不同程度的抑制ADP诱导的新西兰大白兔血小板聚集的作用 ,其中化合物 (4 )的活性最强 ,比先导化合物CCI 17810大约强一倍 ,化合物 (1) ,(2 ) ,(11)也有较强的活性 .
Analogues of 6 〔(4 substituted piperazine)phenyl〕 4,5 dihydro (2 H )pyridazinones were synthesized in searching for more potent and selective antithrombotic drugs.All the title compounds were first reported.The results of preliminary pharmacological tests showed that all the compounds synthesized had activities against platelet aggregation induced by ADP in vitro in rabbits.Compound (4) was the most potent.Compound (1),(2),(11) had potent activities too.SAR were also discussed.
出处
《中国药物化学杂志》
CAS
CSCD
2000年第4期254-257,共4页
Chinese Journal of Medicinal Chemistry
