Structure-based design,synthesis of novel inhibitors of Mycobacterium tuberculosis FabH as potential anti-tuberculosis agents  

作　　者：Xue Hui Zhang Hong Yu Wu Zhong Li LiWang Song Li 

机构地区：[1]Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China [2]Drug Evaluation Center of State Food and Drug Administration, Beijing 100038, China

出　　处：《Chinese Chemical Letters》2009年第9期1019-1022,共4页中国化学快报（英文版）

基　　金：supported by the National Basic Research Program of China(No.2004CB518908);the National High Technology Research and Development Program of China(No.2006AA020601)

摘　　要：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. 2009 Song Li. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.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. 2009 Song Li. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.

关 键 词：Structure-based design SYNTHESIS Enzyme inhibitor Mycobacterium tuberculosis FabH 

分 类 号：S858.23[农业科学—临床兽医学] Q946.88[农业科学—兽医学]