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.
出处
《化学世界》
CAS
CSCD
北大核心
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)
关键词
包甲素类似物
M胆碱能激动剂
合成
analogs of Baogongteng A
muscarinic cholinergic agonist
synthesis
