噻吩并四氢吡啶衍生物的合成及其抗血小板聚集活性研究  

Synthesis of thienopyridine derivatives and its anti-platelet activity in vivo

作　　者：周云松[1,2] 王平保[2] 刘颖[2] 陈继方[3] 岳南[2] 刘登科[2] 

机构地区：[1]天津医科大学研究生院,天津300070 [2]天津药物研究院,天津300193 [3]天津工业大学环境与化学工程学院,天津300160

出　　处：《药学学报》2011年第1期70-74,共5页Acta Pharmaceutica Sinica

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

摘　　要：为了寻找新型的ADP受体拮抗剂类抗血栓药物,合成了18个未见文献报道的噻吩并四氢吡啶衍生物,化合物结构经1H NMR和MS确证。大鼠体内抗血小板聚集活性研究表明,化合物C1的活性优于阳性对照药噻氯匹定,值得进一步深入研究;化合物A4、B2、C4和C7均有不同程度的抑制血小板聚集的活性。To explore novel ADP receptor inhibitors with anti-thrombotic activity,eighteen compounds were synthesized and their structures were confirmed by 1H NMR and MS.The results showed that the activity of compound C1 was superior to ticlopidine in platelet aggregation inhibition tests in vivo and worthy for further investigation.Compounds A4,B2,C4 and C7 possessed moderate platelet aggregation inhibitory activities.

关 键 词：噻吩并四氢吡啶衍生物 合成 ADP受体拮抗剂 抗血小板聚集 

分 类 号：R916[医药卫生—药学]