红霉素衍生物的成环修饰  

Cyclization Strategies in Modification of Erythromycin Derivatives

作　　者：张峰[1] 毕小玲[1] 

机构地区：[1]中国药科大学药物化学教研室,江苏南京210009

出　　处：《药学进展》2010年第6期241-248,共8页Progress in Pharmaceutical Sciences

摘　　要：半合成红霉素衍生物是临床上一类重要的抗感染药物,但细菌对现有品种产生日益严重的耐药性,因此急需研发出对耐药菌有效的新型大环内酯类抗生素。在深入研究抗菌作用机制的基础上,对红霉素的化学结构进行修饰与改造,特别是通过环状体系的引入与变换这一有效的药物设计方法,已获得了很多结构新颖且具有较强抗菌活性的红霉素衍生物。综述近年来在红霉素衍生物成环修饰方面的进展,重点介绍若干具有优良抗菌活性的新化合物以及相关的构效关系信息。Semi-synthetic erythromycin derivatives represent an important class of anti-infective agents in clinical therapy.Meanwhile,the prevalent resistance to the marketed macrolides drives the rapid deve-lopment of novel macrolide antibiotics to address bacterial resistance.Thus the extensive structure modifications of erythromycin have been carried out based on the in-depth investigations into the interaction of macrolides with the target ribosome.It is noted that the cyclic system transformation,an effective strategy in drug design,is widely adopted,leading to the emergence of a number of new macrolide derivatives active against susceptible or resistant pathogens.This review summarized the recent advances in cyclization modification of erythromycin scaffold,and introduced some promising erythromycin derivatives with high antibacterial activity.Some relevant structure-activity relationship information was also provided.

关 键 词：红霉素 成环修饰 酮内酯 二氮内酯 

分 类 号：R917[医药卫生—药物分析学]