新型含哌嗪的噻吩并四氢吡啶衍生物的合成及其抗血小板聚集活性  

Synthesis and Anti-platelet Aggregation Activities in vivo of Novel Tetrahydrothienopyridine Derivatives with Piperazine

作　　者：支爽[1] 郑帼[2] 刘颖[3] 王景阳[3] 刘登科[3] 

机构地区：[1]天津工业大学环境与化学工程学院,天津300160 [2]天津工业大学天津市纺织纤维界面处理技术工程中心,天津300160 [3]天津药物研究院天津市新药设计与发现重点实验室,天津300193

出　　处：《合成化学》2011年第6期730-733,共4页Chinese Journal of Synthetic Chemistry

基　　金：国家"重大新药创制"科技重大专项项目(2009ZX09103-078);天津市科技计划项目(09ZCKFSH01300)

摘　　要：运用生物电子等排及药物代谢原理,设计并合成了8个新型的含哌嗪的噻吩并四氢吡啶类衍生物(4a～4h),产率85.5%～91.3%,其结构经1H NMR和HR-MS表征。大鼠体内血小板聚集模型评价测试结果表明,4a～4h均有一定抗血小板聚集活性,其中4c和4e的活性明显优于阳性对照药噻氯匹定,抑制率分别为75.9%和67.4%。Eight novel tetrahydrothienopyridine derivatives（4a- 4h, yield of 85.5% - 91.3% ） withpiperazine were designed and synthesized by bioisosterism and principles of drug metabolism. The structures were characterized by ^1H NMR and HRMS. The anti-platelet aggregation activities were evaluated by platelet aggregation inhibition tests in rats. The results showed that 4a -4h exhibited certain anti-platelet aggregation activities. Compared with the positive control ticlopidine, 4e and 4e exhibited obvious platelet aggregation inhibition, 75.9% and 67.4%, respectively.

关 键 词：噻吩并四氢吡啶 哌嗪 合成 抗血小板聚集活性 

分 类 号：O626.4[理学—有机化学] R914.5[理学—化学]