Research progress in the structural modification of ketolides
10.16438/j.0513-4870.2018-0238
- VernacularTitle:酮内酯抗生素结构修饰的研究进展
- Author:
Xiao-xi ZHANG
1
;
Shuang YANG
1
;
Zhe-hui ZHAO
1
Author Information
1. Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
- Publication Type:SPECIAL REPORTS
- Keywords:
macrolide;
ketolide;
telithromycin;
structural modification
- From:
Acta Pharmaceutica Sinica
2018;53(6):852-864
- CountryChina
- Language:Chinese
-
Abstract:
Macrolide antibiotics have been widely utilized in the treatment of bacterial infections due to their strengths, low toxicity, and high efficacy. Because of the widespread application of macrolide drugs, the emergence of antibacterial resistance against antibiotics has become prominent. Ketolides, as the third generation macrolides, display improvement in activities against macrolide-resistant pathogens with broad antibacterial spectrum. Due to hepatotoxicity, the use of telithromycin has been limited. It is urgent to identify the novel sources of ketolides. So the structural modification of ketolides become the main research field of macrolide. This review introduces the recent progress in the structural modification of ketolide, with the purpose of providing support to development of new ketolide antibiotics.