Synthesis and in vitro antitubercular evaluation of novel sansanmycin derivatives |
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Authors: | Li Yang-Biao Xie Yun-Ying Du Na-Na Lu Yu Xu Hong-Zhang Wang Bin Yu Ying Liu Yan-Xin Song Dan-Qing Chen Ru-Xian |
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Institution: | Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. |
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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. |
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Keywords: | Sansanmycin Antitubercular Structure-activity relationship Uridyl peptide Drug-resistance |
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