新型N-取代四氢噻吩并[3,2-c]吡啶类衍生物的合成及其抗血小板聚集活性  

Synthesis and Anti-platelet Aggregation Activities of Novel N-substituted-tetrahydrothienopyridine Derivatives

作　　者：刘颖[1,2] 陈立功[1] 廖上腾[2] 刘登科[2] 

机构地区：[1]天津大学化工学院,天津300072 [2]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》2013年第4期387-392,共6页Chinese Journal of Synthetic Chemistry

基　　金：国家科技重大专项"重大新药创制"课题资助项目(2013ZX09102014)

摘　　要：以4,5,6,7-四氢噻吩并[3,2-c]吡啶为起始原料,设计并合成了一系列新型的含哌嗪结构的噻吩并吡啶类化合物(3a～3p),其结构经1H NMR,13C NMR,IR和ESI-HR-MS表征。大鼠体内抗血小板聚集活性研究表明,3a～3p均具有一定的抗血小板聚集作用,其中3a,3c,3i和3j的抑制率分别为66.8%,69.5%,70.4%和65.2%。A series of novel piperazine-bearing thienopyridine derivatives（3a～3p） were designed and synthesized from 4,5,6,7-tetrahydrothienopyridine.The structures were characterized by 1H NMR,13C NMR,IR and ESI-HR-MS.In vivo anti-platelet aggregation tests in rats showed that 3a～3p exhibited certain anti-platelet aggregation activities.The inhibitions of 3a,3c,3i and 3j were 66.8%,69.5%,70.4% and 65.2%,respectively.

关 键 词：噻吩并吡啶 哌嗪 合成 抗血小板聚集活性 

分 类 号：O621.3[理学—有机化学] R914.5[理学—化学]