利福霉素类抗生素及其构效关系研究进展  

An update on progress in candidates and structure-activity relationships of the rifamycins

作　　者：罗忠枚[1] 夏小冬[1] 崔玉彬[1] 蒋晓磊[1] 马超[1] 曹胜华[1] 

机构地区：[1]中国医药集团总公司四川抗菌素工业研究所,成都610052

出　　处：《中国抗生素杂志》2012年第4期308-319,共12页Chinese Journal of Antibiotics

摘　　要：本文综述了抗结核病利福霉素类抗生素的不同结构修饰方法、构效关系(SAR)及其典型衍生物。同时,本文阐述了这些衍生物体内外抗结核分枝杆菌(MTB)活性,甚至包括一些候选药物的临床试验结果。其中重点讲述了利福平、利福布汀和利福拉齐的结构修饰衍生物,而目前利福布汀和利福拉齐的衍生物是近年利福霉素类抗结核药物研究的热点,发现了一些有较好开发前景的新候选物,如RFA-2和RFA-2,且利福平衍生物rifalong和利福霉素类杂合物也值得关注。This article reviewed structure-actiVity relationships（SAR）, lots of modifications and the typical derivatives of the rifamycins for tuberculosis. What＇s more, it disclosed in vitro and in vivo activity against Mycobacterium tuberculosis （MTB） of the derivatives, as well as clinical trial results of some drug candidates. And it focused on the modifications of rifampicin, rifabutin and rifalazil, when the active topics of the rifamycins as anti- Tuberculosis drugs were the derivatives of rifabutin and rifalazil in recent years with discovering some promising active compounds, such as RFA-1 and RFA-2. In addition, a rifampicin derivative rifalong and novel rifamycin hybrids were to be mentioned because of their potential activities.

关 键 词：利福霉素 结核病 结核分枝杆菌 多耐药结核分枝杆菌 构效关系(SAR) 

分 类 号：R978.991[医药卫生—药品]