新一代红霉素衍生物及其构效关系研究进展

综述国内外关于十四元大环内酯类抗生素红霉素的结构修饰和所得衍生物抗菌活性的研究近况,介绍了若干个有较好抗菌活性的先导化合物。大环内酯类抗生素广泛应用于临床的同时,细菌对其产生耐药性的问题也愈发突出。以酮内酯为代表的新一代大环内酯类红霉素衍生物具有良好的药动学性质,且对耐药菌有很好的活性,成为近年来大环内酯类抗生素研发的重点。

Recent Progress in Studies on New Generation Erythromycin Derivatives and Their Structure-activity Relationship

The recent progress in studies on the structure modification of 14-mernbered semisynthetic erythromycin and antimicrobial activity of the related derivatives was summarized. Several promising lead compounds were introduced. Macrolide antibiotics have been widely used in clinic, but the macrolide resistance acquired by a variety of pathogens has reached an alarming level consequently. The novel generation maerolide erythromycin derivatives have shown the improved pharmacokinetics profiles and the high activity against resistant strains, in which ketolides are the representative compounds, thus become the development emphasis for macrolide antibiotics.