包公藤甲素类似物的研究  

Analogs of Baogongteng A

作　　者：宋晓宏[1] 王惠宁[1] 姚天荣[1] 

机构地区：[1]上海第二医科大学,上海铁道医院

出　　处：《中国药学杂志》1995年第3期168-171,共4页Chinese Pharmaceutical Journal

摘　　要：本实验设计合成了包公藤甲素类似物１４个，对莨菪烷骨架上的Ｃ＿３，Ｃ＿６和Ｎ＿８取代基团作了结构修饰。初步药理结果表明，其中３个具有抗胆碱作用，２个具有拟胆碱作用，并探讨了莨菪类化合物对Ｍ受体作用的构效关系。Fourteen analogs of Baogongteng A were designed and synthesized.The tropaneskeleton of the compounds was not changed, while the substituting groups of the C_3,C_6and N_8were modified. The results of pharmacological screening showed that 3a-hydroxy-6β-acetoxynortropane and 3α-cinnamoyloxy-6β-acetoxy nortropane possess cholinergic aetivities, while 3abenzoyloxy-6β-acetoxy tropane, 3α-parachlorobenzoyloxy-6β-acetoxy tropane and 3aparani-trobenzoyloxy-6β-acetoxy tropane have anticholinergic activities。 The activity-structure reletion-ships between the tropane compounds and their effects on M-receptor were discussed。

关 键 词：包公藤甲素 拟胆碱能 抗胆碱能 包公藤 药物化学 

分 类 号：R284.1[医药卫生—中药学]