Design,synthesis and antimycobacterial activity of less lipophilic Q203 derivatives containing alkaline fused ring moieties |
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| Authors: | Apeng Wang Hongjian Wang Yunhe Geng Lei Fu Jian Gu Bin Wang Kai Lv Mingliang Liu Zeyu Tao Chao Ma Yu Lu |
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| Affiliation: | 1. Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China;2. College of Chemistry and Material Science, Hebei Normal University, Shijiazhuang 050024, China;3. Beijing Key Laboratory of Drug Resistance Tuberculosis Research, Department of Parmacology, Beijing Tuberculosis and Thoracic Tumor Research Institute, Beijing Chest Hospital, Capital Medical University, Beijing 101149, China;4. College of Pharmacy, Southwest Minzu University, Chengdu 610041, China |
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| Abstract: | We report herein the design and synthesis of a series of less lipophilic Q203 derivatives containing an alkaline fused ring moiety. Most of them show considerable potency against MTB H37Rv strain (MIC?13, 15, 19, 21, 23, 25, 29, 35, 36) have the same excellent activity against both drug-sensitive and -resistant strains (MIC?29 also displays acceptable safety, greater absorption in plasma and aqueous solubility than Q203, suggesting its promising potential to be lead compound for future antitubercular drug discovery. |
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| Keywords: | Tuberculosis Pharmacokinetics Structure-activity relationship |
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