title: Synthesis and in vitro antitubercular evaluation of novel sansanmycin derivatives.
abstract: Tuberculosis (TB) is a major health problem worldwide. A series of novel sansanmycin derivatives were designed, semi-synthesized and evaluated for their activity against drug-susceptible Mycobacterium tuberculosis strain H(37)Rv with sansanmycin A (SSA) as the lead. Among these analogs tested, compound 1d possessing an isopropyl group at the amino terminal afforded an increased antimycobacterial activity with a MIC value of 8 μg/mL in comparison with SSA. Importantly, it was active for rifampicin- and isoniazid-resistant M. tuberculosis strain isolated from patients in China. These promising results offer an opportunity for further exploration of this novel class of analogs as antitubercular agents.
authors: Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
authors: Yang-Biao
authors: YB
authors: Li
authors: Yun-Ying
authors: YY
authors: Xie
authors: Na-Na
authors: NN
authors: Du
authors: Yu
authors: Y
authors: Lu
authors: Hong-Zhang
authors: HZ
authors: Xu
authors: Bin
authors: B
authors: Wang
authors: Ying
authors: Y
authors: Yu
authors: Yan-Xin
authors: YX
authors: Liu
authors: Dan-Qing
authors: DQ
authors: Song
authors: Ru-Xian
authors: RX
authors: Chen
mesh_terms: D000995:Antitubercular Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002681:China; D006801:Humans; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D009842:Oligopeptides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013302:Streptomyces / Q000737:chemistry; D014376:Tuberculosis / Q000188:drug therapy*; D018088:Tuberculosis, Multidrug-Resistant; D014529:Uridine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000995:Antitubercular Agents; D009842:Oligopeptides; C519865:sansanmycin; D014529:Uridine