2005
DOI: 10.1021/jm049141s
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Structure-Based Design, Synthesis, and Study of Potent Inhibitors of β-Ketoacyl-acyl Carrier Protein Synthase III as Potential Antimicrobial Agents

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-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 to be candidates within a novel class of s… Show more

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Cited by 98 publications
(85 citation statements)
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“…The cassettes were flanked by ϳ1 kb of homologous DNA flanking the fabY gene in P. aeruginosa PAO1. Vectors were mobilized in trans using E. coli Stellar cells (Clontech) transformed with the helper plasmid pRK2013 (16) as the conjugation-proficient donor strain along with different recipient P. aeruginosa strains as has been described previously (56). Merodiploid colonies were confirmed by colony PCR and outgrown for 4 h in 1 ml of LB only at 37°C.…”
mentioning
confidence: 99%
“…The cassettes were flanked by ϳ1 kb of homologous DNA flanking the fabY gene in P. aeruginosa PAO1. Vectors were mobilized in trans using E. coli Stellar cells (Clontech) transformed with the helper plasmid pRK2013 (16) as the conjugation-proficient donor strain along with different recipient P. aeruginosa strains as has been described previously (56). Merodiploid colonies were confirmed by colony PCR and outgrown for 4 h in 1 ml of LB only at 37°C.…”
mentioning
confidence: 99%
“…FabH, a β-ketoacyl-acyl carrier protein synthase, is the bacterial condensing enzyme in Gram-positive and Gram-negative bacteria that initiates the cycle by catalyzing the first condensation step between acetyl-CoA and malonyl-ACP (139,140). Mycolic acid, one of the structurally largest fatty acids found in nature, is a vital cell wall component of the human tuberculosis strain of Mycobacterium tuberculosis.…”
Section: Thiolactomycin : Bacterial Fatty Acid Synthesis Inhibitormentioning
confidence: 99%
“…Significant studies in this area have been made by Thomas et al 13 who described an asymmetric synthesis of 5,5΄-disubstituted thiotetronic acids using a [3,3] rearrangement of an allyl xanthane to the corresponding dithiocarbonate. Recently, Townsend et al 14 described a flexible route to (5R)-thiolactomycin employing Seebach's self-regenaration of chirality method.…”
Section: 11mentioning
confidence: 99%