新一代大环内酯类抗生素——酮内酯类简介

A Brief Introduction on Macrolides Antibiotics of Novel Generation Ketolides

大量耐药病原菌的迅速出现加速了寻找新抗生素的步伐,近年来研制出一种经结构修饰的大环内酯类衍生物,即酮内酯。酮内酯是把14元大环内酯C-3上的红霉糖基替换为羰基而得到的新一类抗生素。现综述大环内酯的获得性耐药机制,进而阐明以大环内酯为基础经结构改造而来的酮内酯类抗生素的构效关系,并介绍其代表性药物泰利霉素和喹红霉素(ABT-773)的临床特性。

The rapid emergence of drug resistance in many pathogenic bacteria intensified the search for new antimicrobial agents.which led to the development of chemically modified macrolides,namely,the ketolides ketolides are a novel class of antibiotics derived from 14-membered macrolides by substitution of the cladinose sugar by a 3-keto group. The mechanism of acquired macrolide resistance,the structureactivity relationships of ketolides and clinical properties of cethromycin （ABT-773） and telithromycin are mainly stated in this review.