Potent, Novel in Vitro Inhibitors of the Pseudomonas a eruginosa Deacetylase LpxC

…, NH Andersen, EA Harwood, J Bowman…

Index: Kline, Toni; Andersen, Niels H.; Harwood, Eric A.; Bowman, Jason; Malanda, Andre; Endsley, Stephanie; Erwin, Alice L.; Doyle, Michael; Fong, Susan; Harris, Alex L.; Mendelsohn, Brian; Mdluli, Khisimuzi; Raetz, Christian R. H.; Stover, C. Kendall; Witte, Pamela R.; Yabannavar, Asha; Zhu, Shuguang Journal of Medicinal Chemistry, 2002 , vol. 45, # 14 p. 3112 - 3129

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Citation Number: 92

Abstract

Deacetylation of uridyldiphospho-3-O-(R-hydroxydecanoyl)-N-acetylglucosamine by LpxC is the first committed step in the Pseudomonas aeruginosa biosynthetic pathway to lipid A; homologous enzymes are found widely among Gram-negative bacteria. As an essential enzyme for which no inhibitors have yet been reported, the P. aeruginosa LpxC represents a highly attractive target for a novel antibacterial drug. We synthesized several focused ...