酮内酯抗生素结构修饰的研究进展  

Research progress in the structural modification of ketolides

作　　者：张晓曦 杨爽 赵哲辉 ZHANG Xiao-xi;YANG Shuang;ZHAO Zhe-hui(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)

机构地区：[1]中国医学科学院、北京协和医学院药物研究所,活性物质发现与适药化研究北京市重点实验室,北京100050

出　　处：《药学学报》2018年第6期852-864,共13页Acta Pharmaceutica Sinica

摘　　要：大环内酯类抗生素因其安全性较好,抗菌活性高,多年来用于治疗呼吸系统感染等疾病。但由于近年来抗生素的广泛使用,细菌耐药现象也越来越严重。酮内酯作为第三代大环内酯类抗生素对耐药菌显示出突出的活性,同时还能保持大环内酯的宽抗菌谱。但酮内酯的代表药物——泰利霉素因存在肝毒性,其适应症受到限制,寻找新的酮内酯抗生素刻不容缓,因此酮内酯的研究逐步成为大环内酯类抗生素的主要研究部分,本文对近年来酮内酯的结构修饰研究进行了综述,希望能对研发酮内酯新药有所帮助。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.

关 键 词：大环内酯 酮内酯 泰利霉素 结构修饰 

分 类 号：R916[医药卫生—药学]