毒扁豆碱类似物抑制胆碱酯酶构效关系的研究  

Studies on Relationship Between the Structures of Physostigmine Analogues and their Anticholinesterase Activities

作　　者：王明亮 傅辛福 戴永健 徐仁 

机构地区：[1]海军医学高级专科学校药品检验系

出　　处：《中国药物化学杂志》1997年第1期59-62,共4页Chinese Journal of Medicinal Chemistry

摘　　要：测定了２９个毒扁豆碱类似物的抑制胆碱酯酶活性，对其结构与抑酶活性强度、抑制时间及毒性之间的关系进行了探讨，结果表明：（１）去掉毒扁豆碱的第二个并吡咯环可保持抑酶活性并降低毒性和延长作用时间．（２）胺甲酰氧侧链氮原子上选用较长碳链烷基亦可保持抑酶活性并降低毒性和延长作用时间．（３）二氢吲哚环１位和３位选择较小的烷基取代基时活性较高．The anticholinesterase activity of 29 physostigmine analogues were determined.Relationship between structure and inhibition,duration of action and toxicity was studied.Three major conclusions are apprent from this study.First,the second pyrrole ring is not necessary for cholinesterase inhibition.Long lasting duration of action and low toxicity would be achieved without it.Second,the methylcarbamoyl group can be substituted by longer monoalkylcarbamoyl groups.They can also assure longer lasting action and lower toxicity.Third,the short alkyl groups in C 1 and C 3 postition are important to great inhibition.

关 键 词：毒扁豆碱类似物 抑制作用 胆碱酯酶 化学药理学 

分 类 号：R962[医药卫生—药理学]