基于酚类中药活性小分子先导化合物的合成设计  

Design and Synthetic of Active Small Phenols Molecule as the Lead Compounds of Chinese Herbal Medicine

作　　者：牛倩[1] 孙鹏[1,2] 葛德助 丁连峰 张言鹏[3] 李玉祥[3] 

机构地区：[1]亳州职业技术学院药学院,安徽亳州236800 [2]亳州市中药研究所,安徽亳州236800 [3]安徽济人药业有限公司,安徽亳州236800

出　　处：《广州化工》2016年第17期28-29,37,共3页GuangZhou Chemical Industry

基　　金：安徽省质量工程项目药品质量检测技术特色专业(2014tszy055);安徽省高校省级科学研究项目(KJ2013Z219)

摘　　要：酚类化合物是一类比较常见的中药活性小分子先导化合物,在生物机体内起着重要的生命调控作用,参与了生命过程中的许多反应。此类化合物因本身理化性质等方面的限制,成药指数低制约了本类成分的后续开发。利用药物设计理论结合酚类有机物的化学性质,讨论分析烃基化、羟基酰化成酯、羟基卤代、成盐、建立桥键等酚类中药活性小分子修饰方法,可为遴选有效的酚类天然药物活性成分提供思考。Phenolic compounds is a kind of common active small molecule as the lead compounds,plays an important role in the regulation of life organism,is involved in many reactions in the course of life. The development of this kind of compounds is slow because of their physical and chemical properties,etc. Using the theory of drug design,according to the chemical properties of organic compounds,design and synthetic of active small phenols molecule as the lead compounds of Chinese herbal medicine by alkylation,acylation into esters,halogenated hydroxy,salt,bridge bond,etc.,were discussed,to provide effective selection references for the phenolic natural medicine active ingredients.

关 键 词：酚类中药活性小分子 先导化合物 合成设计 

分 类 号：R914.2[医药卫生—药物化学] O621.3[医药卫生—药学]