3-取代-6β-乙酰氧基莨菪烷的合成及其生物活性研究  

Synthesis and Bioactivities of 3α-Substituted-6β-acetoxytropane Derivatives

作　　者：钮因尧[1] 杨丽敏[1] 崔永耀[1] 朱亮[1] 冯菊妹[1] 陈红专[1] 陆阳[1] 

机构地区：[1]上海第二医科大学药物研究所,上海200025

出　　处：《化学世界》2005年第5期299-301,295,共4页Chemical World

基　　金：上海市教委学科建设专项基金资助项目(JY2001)

摘　　要：以3α羟基6β乙酰氧基莨菪烷(5)为起始原料,合成4个新3 取代6β乙酰氧基莨菪烷。药理筛选结果表明3α苯磺酰氧基6β乙酰氧基莨菪烷(6d)对大鼠回肠肌具有强激动活性;经M受体阻断剂阿托品的拮抗试验,提示6d是潜在的M胆碱能受体激动剂。Four new 3α -substituted-6β-acetoxytropane derivatives were synthesized from 3α-hydroxy-6β-acetoxytropane. The results of preliminary pharmacological tests showed that 3α -benzensulfonyloxy- 6β -accetoxytropane (6d) had strong agonistic effect on ileal muscle of guinea-pigs. Since this agonistic effect was blocked by atropine, an exclusive muscarinic-receptor antagonist, it suggested that 6d was a potential muscarinic cholinergic agonist.

关 键 词：包甲素类似物 M胆碱能激动剂 合成 

分 类 号：R988.1[医药卫生—药品]