二氢哒嗪酮类化合物的合成及其抗血小板聚集活性研究  

Synthesis and antiplatelet aggregation activity of dihydropyridazinone derivatives

作　　者：倪瑾[1] 蔡灵芝[2] 俞世冲[2] 蔡建明[1] 徐建明[2] 吴秋业[2] 

机构地区：[1]第二军医大学海军医学系防原医学教研室,上海200433 [2]第二军医大学药学院有机化学教研室,上海200433

出　　处：《药学服务与研究》2007年第3期198-201,共4页Pharmaceutical Care and Research

基　　金：上海市长宁区科委资助课题(No.20054Y17001)

摘　　要：目的:合成新的哒嗪酮类化合物,并研究其抗血小板聚集活性。方法:在6-(4-氯乙酰氨基苯基)-4,5-二氢-3(2H)-哒嗪酮侧链引入不同取代的哌嗪,合成了一系列化合物,采用1H-NMR、IR及元素分析等方法确证其结构。采用Born比浊法进行体外抗血小板聚集药理实验。结果:合成的10个化合物都具有一定的抗血小板凝集的活性,其中化合物4的抗血小板聚集活性明显优于先导化合物MCI-154。结论:4-位取代哌嗪环基的引入对哒嗪酮类化合物抗血小板聚集的活性有显著影响。Objective： To synthesize new pyridazinone derivatives and study their antiplatelet aggregation activity. Methods： A series of compounds were synthesized by introducing different piperazine groups in side chain of 6-（4-chloro- acetamido-phenyl）-4,5-dihydro-3（2H）-pyridazinones. The chemical structures of all the target compounds were confirmed by 1 H-NMR,IR and elemental analysis. Born＇s turbidimetry was applied for preliminary antiplatelet aggregation pharmacological test in vitro. Results： The preliminary pharmacological test showed that all the target compounds exhibited potent antiplatelet aggregative activity to a certain extent. The inhibitory activity of platelet aggregation of compound 4 was significantly stronger than that of lead compound MCI-154. Conelusion： Inletting different substituting piperazine groups can obviously enhance antiplatelet aggregation activity of pyridazinone derivatives.

关 键 词：化学 有机 哒嗪类 血小板聚集抑制剂 体外研究 

分 类 号：R916.42[医药卫生—药学] R973.2