丁公藤碱Ⅱ类似物的合成及其生物活性  

THE SYNTHESIS AND PHARMACOLOGICAL ACTIVITIES OF ANALOGS OF ERYCIBE ALKALOID Ⅱ

作　　者：何虎明 沈家祥[1] 马秀英[2] 何湘萍[2] 

机构地区：[1]北京医科大学药学院 [2]军事医学科学院毒物药物研究所,北京100850

出　　处：《药学学报》1989年第5期335-340,共6页Acta Pharmaceutica Sinica

基　　金：高校科学基金

摘　　要：本文设计合成了丁公藤碱Ⅱ的C_2脱氧和C_8电子等排类似物。药理结果表明,丁公藤碱Ⅱ的C_2羟基是保持其缩瞳活性的关键部分之一;目的物2和4各自分别具有拟和抗胆碱活性;电子等排目的物16和17既无拟也无抗胆碱作用。The C_2 deoxy and C_6 electron isosterie analogs of a new antiglaucoma agent, erycibe alkaloid Ⅱ, were designed and synthesized. The main pharmacological results were as follows: 1. The C_2-OH in erycibe alkaloid Ⅱ was one of the key groups for its myotic activity; 2. It was worth noting that compounds 2 and 4 showed cholinergie and anticholinergic activities, respectively. This phenomenon in tropane alkaloids was not reported before; 3. The C_6 electron isosteric compounds 16 and 17 showed neither anticholinergic nor cholinergic activities.

关 键 词：丁公藤碱II 拟胆碱能活性 生物碱 

分 类 号：R914.5[医药卫生—药物化学]