红霉素衍生物抗菌活性构效关系研究进展

Recent development in the structure-activity relationships for the antimicrobial activity of erythromycin derivatives

为解决抗生素的耐药性问题,近年来在红霉素化学结构修饰方面开展了大量的研究,并发现了诸如酮内酯、酰内酯、双环内酯等多种具有良好抗耐药菌活性的新型大环内酯类化合物。该文对红霉素衍生物抗菌活性研究成果做一概括,并对构效关系研究的某些重要结论加以探讨。

To address the problem of antibiotic resistance, tremendous efforts had been devoted to the chemical modification of erythromycin during the past several years. As a consequence, several novel series of macrolides, such as ketolide, acylide, bicyclolide, etc., had been recognized to be highly effective against macrolide-resistant pathogens. In this review, the recent progress on the antimicrobial research area of erythromycin derivatives were summarized and some important conclusions regarding structure-activity relationships were also discussed.