6-(4-取代苯基)-5-甲基-4,5二氢-3(2H)哒嗪酮类化合物的合成及其抑制血小板聚集作用  

Synthesis and platelet aggregation inhibition activity of analogues 6-4-(substituted phenyl)-5-methyl-4,5-dihydro-3(2H)-pyridazinones

作　　者：覃军[1] 王祥智[1] 刘毅敏[1] 肖湘[1] 刘海红[1] 成晓玲[2] 

机构地区：[1]第三军医大学化学教研室 [2]第三军医大学西南医院输血科,重庆400038

出　　处：《化学研究与应用》2006年第9期1088-1091,共4页Chemical Research and Application

摘　　要：血小板聚集在血栓形成中起着先导而关键的作用，而严重威胁人类生命健康的心脑血管疾病多数与血栓形成和血栓栓塞有着密切的联系。二氢哒嗪酮类化合物对抑制血小板聚集有较强的药理活性，对二磷酸腺苷（ADP）、花生四烯酸（AA）、血小板活化因子（PAF）和胶原（Collagen）引起的血小板聚集均有抑制作用。深入研究二氢哒嗪酮类化合物的构效关系，以期寻找活性更强的抗血小板聚集药物，是开发新型心脑血管系统疾病药物的重要研究方向之一。本文设计合成了6-（4-取代苯基）-5-甲基4，5二氢-3（2H）哒嗪酮类化合物，并进行了体外药理实验。The 6-4 （ substituted phenyl） -5-methyl-4,5-dihydro-3 （ 2H ） -Pyridazinones were designed and synthesized for searching more potent platelet aggregation inhibitor. A series of reactions, such as Friedel-Crafts acylation reaction, cyanidation,hydrolysis, cyclation were used to synthesize the title compounds. The structures of all title compounds synthesized were confirmed by i H NMR, MS, IR, and element analysis. Results of pharmacological test showed that four compounds synthesized have the potent inhibition activities against the human platelet aggregation induced by adenosine diphosphate（ADP）in vitro.

关 键 词：哒嗪酮 化学合成 血小板聚集 

分 类 号：TQ463.54[化学工程—制药化工]