PMID:19836235
| Citation |
Lv, PC, Wang, KR, Yang, Y, Mao, WJ, Chen, J, Xiong, J and Zhu, HL (2009) Design, synthesis and biological evaluation of novel thiazole derivatives as potent FabH inhibitors. Bioorg. Med. Chem. Lett. 19:6750-4 |
|---|---|
| Abstract |
Fatty acid biosynthesis is essential for bacterial survival. Components of this biosynthetic pathway have been identified as attractive targets for the development of new antibacterial agents. FabH, beta-ketoacyl-acyl carrier protein (ACP) synthase III, is a particularly attractive target, since it is central to the initiation of fatty acid biosynthesis and is highly conserved among Gram positive and negative bacteria. Three series of Schiff bases containing thiazole template were synthesized and developed as potent inhibitors of FabH. This inhibitor class demonstrates strong antibacterial activity. Escherichia coli FabH inhibitory assay and docking simulation indicated that the compounds 11 and 18 were potent inhibitors of E. coli FabH. |
| Links |
PubMed Online version:10.1016/j.bmcl.2009.09.111 |
| Keywords |
3-Oxoacyl-(Acyl-Carrier-Protein) Synthase/antagonists & inhibitors; Anti-Bacterial Agents/chemical synthesis; Anti-Bacterial Agents/chemistry; Anti-Bacterial Agents/pharmacology; Drug Design; Enzyme Inhibitors/chemical synthesis; Enzyme Inhibitors/chemistry; Enzyme Inhibitors/pharmacology; Gram-Negative Bacteria/drug effects; Gram-Negative Bacteria/enzymology; Gram-Positive Bacteria/drug effects; Gram-Positive Bacteria/enzymology; Microbial Sensitivity Tests; Molecular Structure; Stereoisomerism; Thiazoles/chemical synthesis; Thiazoles/chemistry; Thiazoles/pharmacology |
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