新型N-取代-2-(2-氯苯基)-2-｛6,7-二氢噻吩并[3,2-c]吡啶-5(4H)-基｝乙酰胺的合成及其抗血小板聚集活性  

Synthesis and Antiplatelet Aggregation Activities of N-substituted-2-(o-chlorophenyl)-2-{6,7-dihydrothieno pyridine-5(4H)-yl} Acetamides

作　　者：刘颖[1] 支爽[2] 穆帅[3] 成碟[1] 刘登科[1] 

机构地区：[1]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 [2]天津工业大学环境与化学工程学院,天津300160 [3]天津大学化工学院,天津300072

出　　处：《合成化学》2011年第6期718-722,共5页Chinese Journal of Synthetic Chemistry

基　　金：国家科技重大专项"重大新药创制"课题(2009ZX09103-078);天津市科技支撑计划重点项目(09ZCKFSH01300)

摘　　要：以2-(2-氯苯基)-2-{6,7-二氢噻吩并[3,2-c]吡啶5(4H)乙酸甲酯为原料,设计并合成了一系列新型的N-取代-2-(2-氯苯基)-2-{6,7-二氢噻吩并[3,2-c]吡啶-5(4H)-基}乙酰胺(4a～4o),其结构经1H NMR和MS表征。体内初步生物活性测试结果表明,4a～4o均有一定的抗血小板聚集作用,其中4a,4l和4m对大鼠血小板聚集的抑制率分别为60.3%,63.0%和65.1%。A series of novel N-substituted-2-（o-chlorophenyl）-2-{6,7-dihydrothieno pyridine-5（4H）-yl}acetamides（4a～4o） were designed and synthesized from 2-（o-chlorophenyl）-2-{6,7-dihydrothienopyridine-5（4H）methyl acetate.The structures were characterized by 1H NMR and MS.Their in vivo biological activity test indicates that 4a～4o exhibited centain anti-platelet aggregation of rats,the inhibitiob rate of 4a,4l and 4m were 60.3%,63.0% and 65.1%,respectively.

关 键 词：噻吩并吡啶 酰胺 合成 抗血小板聚集活性 

分 类 号：O626[理学—有机化学] R914.5[理学—化学]