A short and efficient synthesis of（Z）-2-substituted-5-（4-（（2-substitued-5-oxoimidazolidin-4-ylidene）methyl）benzamido）ben-zoic acid derivatives（8a-g） as potential type of FabH inhibitors is described.Their st...A short and efficient synthesis of（Z）-2-substituted-5-（4-（（2-substitued-5-oxoimidazolidin-4-ylidene）methyl）benzamido）ben-zoic acid derivatives（8a-g） as potential type of FabH inhibitors is described.Their structures were confirmed by MS,NOE and ~1H NMR.展开更多
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 w...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.展开更多
Our previous work showed that an enoyl-ACP reductase gene fabI1 of Sinorhizobium meliloti was down-regulated in the nifA mutant nodule bacteria. To gain a better understanding of fabI1 gene, a single site insertion mu...Our previous work showed that an enoyl-ACP reductase gene fabI1 of Sinorhizobium meliloti was down-regulated in the nifA mutant nodule bacteria. To gain a better understanding of fabI1 gene, a single site insertion mutant was constructed in this study. The fabI1 mutant was retarded in cell growth, and its ability to grow on media with high concentration of NaCl was reduced. In addition, the mutant was completely defective in swarming phenotype. During symbiosis, the fabI1 mutant had delayed nodule formation on host plants. Despite the fact that FabI1 protein showed 66% identity with another enoyl-ACP reductase FabI2 in S. meliloti, defects in fabI1 were not rescued by the plasmidborne version of fabI2. This indicated the different functions of the two FabI proteins in S. meliloti.展开更多
基金supported by the National High Technology Research and Development Program of China(No2006AA020601)
文摘A short and efficient synthesis of（Z）-2-substituted-5-（4-（（2-substitued-5-oxoimidazolidin-4-ylidene）methyl）benzamido）ben-zoic acid derivatives（8a-g） as potential type of FabH inhibitors is described.Their structures were confirmed by MS,NOE and ~1H NMR.
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)
文摘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.
基金supported by the National Natural Sciences Foundation of China (Grant No. 30770171)Shanghai Natural Sciences Foundation (Grant No. 05ZR14135)National Key Basic Research and Development Program of China (Grant No. 2001CB108901)
文摘Our previous work showed that an enoyl-ACP reductase gene fabI1 of Sinorhizobium meliloti was down-regulated in the nifA mutant nodule bacteria. To gain a better understanding of fabI1 gene, a single site insertion mutant was constructed in this study. The fabI1 mutant was retarded in cell growth, and its ability to grow on media with high concentration of NaCl was reduced. In addition, the mutant was completely defective in swarming phenotype. During symbiosis, the fabI1 mutant had delayed nodule formation on host plants. Despite the fact that FabI1 protein showed 66% identity with another enoyl-ACP reductase FabI2 in S. meliloti, defects in fabI1 were not rescued by the plasmidborne version of fabI2. This indicated the different functions of the two FabI proteins in S. meliloti.
