Synthesis and cardiovascular activity of a new series of cyclohexylaralkylamine derivatives related to perhexiline
作者:Gerard Leclerc、Nicole Decker、Jean Schwartz
DOI:10.1021/jm00348a019
日期:1982.6
A series of 24 cyclohexylaralkylamine derivatives related to perhexiline has been synthesized and screened for cardiovascular activity. All the compounds contained an exocyclic amine which was substituted either by an alkyl, cycloalkyl, or aralkyl group. In the hope of further reducing toxicity, the synthesis of p-tolyl- and p-hydroxyphenyl derivatives 23 and 24 was undertaken. The effect of separating
已经合成了一系列与哌己啉相关的24种环己基烷基胺衍生物,并筛选了其心血管活性。所有化合物都含有被烷基,环烷基或芳烷基取代的环外胺。为了进一步降低毒性,进行了对甲苯基和对羟基苯基衍生物23和24的合成。已经系统地检查了相对于芳核分离环己胺部分的效果。根据以下标准顺序,进行药理学研究,以寻找活性优于哌克西林的化合物:(1)α-肾上腺素分解活性;(2)增加冠状动脉血流量;(3)钙拮抗作用。几种化合物比哌克西林更有效,毒性更低。