4″-O-取代红霉素衍生物的研究进展

Recent Progress in Research on 4″-O-Substituted Erythromycin Derivatives

随着大环内酯类抗生素广泛应用于临床,细菌耐药性的问题日趋严重,因此,开发对耐药菌有效的第3代红霉素衍生物成为目前的研究热点。综述红霉素分子上克拉定糖4″位羟基结构修饰的研究进展,并介绍了若干个对耐药菌具有优良抗菌活性的新型4″-O-取代红霉素衍生物。

The therapeutic utility of macrolides has led to rapid increases in the resistance rates of bacteria isolated clinically. The third-generation erythromycin derivatives overcoming bacterial resistance are the hot research topic. The recent progress in research on the C-4＂ modification of 14- and 15-mem- bered semisynthetic erythromycin and the antimicrobial activity of the related derivatives was reviewed. Several promising 4＂-O-substituted erythromycin derivatives with a high activity against resistant strains were also introduced.