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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
【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。
【Abstract】 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；
【Key words】 analogs of Baogongteng A； muscarinic cholinergic agonist； synthesis；
【Key words】 analogs of Baogongteng A； muscarinic cholinergic agonist； synthesis；
【基金】 上海市教委学科建设专项基金资助项目(JY2001)
- 【文献出处】 化学世界 ,Huaxue Shijie (Chemical World) , 编辑部邮箱 ,2005年05期
- 【分类号】R914.5
- 【被引频次】5
- 【下载频次】99