Cyclic guanidines. 14. Imidazo[1,2-a]thienopyrimidin-2-one derivatives as blood platelet aggregation inhibitors
作者:Fumiyoshi Ishikawa、Akira Kosasayama、Hitoshi Yamaguchi、Yoshifumi Watanabe、Junji Saegusa、Seiichi Shibamura、Kyoko Sakuma、Shinichiro Ashida、Yasushi Abiko
DOI:10.1021/jm00136a005
日期:1981.4
A series of novel 1,2,3,5-tetrahydroimidazo[1,2-a]thieno[2,3-d]-, -[3,2,-d]-, and -[3,4-d]pyrimidin-2-one derivatives has been prepared and tested for the activity of inhibiting platelet aggregation in rats in vitro and ex vivo. These compounds were synthesized through the following reactions: sodium borohydride reduction of 2,4-dichlorothienopyrimidines, followed by ethoxycarbonylmethylation and successive
一系列新颖的1,2,3,5-四氢咪唑并[1,2-a]噻吩并[2,3-d]-,-[3,2,-d]-和-[3,4-d]制备了嘧啶-2-酮衍生物,并在体外和离体中测试了抑制大鼠血小板聚集的活性。这些化合物是通过以下反应合成的:硼氢化钠还原2,4-二氯噻吩并嘧啶类,然后进行乙氧羰基甲基化和连续胺化。发现大多数化合物是有效的血液和血小板聚集抑制剂。结构活性关系表明,内酰胺结构和噻吩环上的亲脂性取代基对化合物与血小板上受体位点的有效相互作用至关重要。在研究的化合物中,1,2,3,5,6,7,8,9-八氢-[1]苯并噻吩并[2,3-d]咪唑[1,