Structure-based design, synthesis, and study of potent inhibitors of β-ketoacyl-acyl carrier protein synthase III as potential antimicrobial agents

…, Y Su, S Margosiak, KS Gajiwala, J Cortez…

Index: Nie, Zhe; Perretta, Carin; Lu, Jia; Su, Ying; Margosiak, Stephen; Gajiwala, Ketan S.; Cortez, Joseph; Nikulin, Victor; Yager, Kraig M.; Appelt, Krzysztof; Chu, Shaosong Journal of Medicinal Chemistry, 2005 , vol. 48, # 5 p. 1596 - 1609

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Citation Number: 95

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, β-ketoacyl-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. Small molecules that inhibit FabH enzymatic activity have the potential ...