Design,synthesis and antimycobacterial activity of 3,5-dinitrobenzamide derivatives containing fused ring moieties |
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| Authors: | Apeng Wang Guocheng Huang Bin Wang Kai Lv Hongjian Wang Zeyu Tao Mingliang Liu Huiyuan Guo Yu Lu |
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| Institution: | 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China;2. Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Pharmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital Medical University, Beijing 101149, China |
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| Abstract: | We report herein the design, synthesis and antimycobacterial activity of 3,5-dinitrobenzamide derivatives containing fused ring moieties. Results reveal that many of the target compounds have considerable in vitro antitubercular activity. Especially, N-((2-(4-fluorophenyl)/N-((2-(3-fluorobenzyl)-1,2,3,4-tetrahydroisoquilin-6-yl)methyl)-3,5-dinitrobenzamides 18a and 20e exhibit potent MIC values of 0.056–0.078?μg/mL against both drug-sensitive Mycobacterium tuberculosis (MTB) H37Rv strain and two clinically isolated multidrug-resistant MTB (MDR-MTB) strains, opening a new direction for further SAR studies. |
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| Keywords: | Tuberculosis MTB H37Rv MDR-MTB 3 5-Dinitrobenzamides Structure-activity relationship |
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