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Structure-based design,synthesis of novel inhibitors of Mycobacterium tuberculosis FabH as potential anti-tuberculosis agents |
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| Authors: | Xue Hui Zhanga Hong Yub Wu Zhonga Li Li Wanga Song Li a Beijing Institute of Pharmacology Toxicology Beijing China b Drug Evaluation Center of State Food Drug Administration Beijing China |
| Institution: | a Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China;b Drug Evaluation Center of State Food and Drug Administration, Beijing 100038, China |
| Abstract: | Mycobacterium tuberculosis FabH,an essential enzyme in mycolic acids biosynthetic pathway,is an attractive target for novel anti-tuberculosis agents.Structure-based design,synthesis of novel inhibitors of mtFabH was reported in this paper.A novel scaffold structure was designed,and 12 candidate compounds that displayed favorable binding with the active site were identified and synthesized. |
| Keywords: | Structure-based design Synthesis Enzyme inhibitor Mycobacterium tuberculosis FabH |
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