N-(2-Phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides containing various amine moieties: Design,synthesis and antitubercular activity |
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| Authors: | Linhu Li Apeng Wang Bin Wang Mingliang Liu Kai Lv Zeyu Tao Chao Ma Xican Ma Bing Han Aoyu Wang Yu Lu |
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| Institution: | Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China; Limin Chemical Co., Ltd., Xinyi 221422, China; 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 100149, China |
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| Abstract: | Seven 2,6-disubstituted N-(2-phenoxy)ethyl imidazo1,2-a]pyridine-3-carboxamide series containing various amine moieties were designed and synthesized as new anti-TB agents. Many of them show excellent in vitro activity against both drug-sensitive MTB strain H37Rv and two MDR-MTB clinical isolates (MIC: < 0.002-0.030 μg/mL). Compounds 2f, 5e and 5g display acceptable safety and pharmacokinetic profiles, opening a new direction for further development. |
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| Keywords: | N-(2-Phenoxy)ethyl imidazo[1 2-a]pyridine Design Synthesis Antimycobacterial activity |
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