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.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2012年第4期308-319,共12页
Chinese Journal of Antibiotics
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)
Rifamycins
Tuberculosis
Mycobacterium tuberculosis
Muti-drug resistant Mycobacterium tuberculosis
Structure-activity relationships（SAR）
