酮内酯类抗生素——泰利霉素和喹红霉素的化学合成

Synthesis of two kinds of ketolides,telithromycin and cethromycin

近年来人们研制出一种新的大环内酯类抗生素,即酮内酯类抗生素。第一代红霉素由于对胃酸的不稳定性,致使了第二代的阿奇霉素、罗红霉素等的出现,而且取得了很好的临床效果。但是近年来抗菌形势更加严峻,促使了第三代酮内酯类的研发,其代表药物为泰利霉素(HMR-3647)和喹红霉素(ABT-773),本文就其合成路线、药效学、构效关系等一一加以介绍。

The acid instability of the first-generation erythromycin has led to the emergence of the second- generation azithromycin and roxithromycin which have achieved good clinical results. As the anti-bacterial situation has become more and more severe in recent years, the third-generation of esters has been developed with Talim （HMR- 3647） and erythromycin quinoline （ABT-773） as its representatives. The purpose of this article is to make an introduction of the synthetic route, efficacy and structure-activity relationships.