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Design, Synthesis and Properties of a Potent Inhibitor of Pseudomonas aeruginosa Deacetylase LpxC

Peng, Yunshan and Dobler, Markus and Patnaik, Anup and Liu, Eugene and Nunez, Jill and Kerrigan, John and Dean, Charles and Mckenney, David and Osborne, Colin and Dzink-Fox, Joann and Bojkovic, Jade and Lilly, Maria-Dawn and Sprague, Elizabeth and Hoffmaster, Keith and Ranjitkar, Srijan and Wang, Bing and hamann, lawrence and tommasi, ruben and glick, meir and yang, xia and wang, honming and parker, david and wattanasin, som and lenoir, francois and Xie, Lili and Yu, Donghui (2017) Design, Synthesis and Properties of a Potent Inhibitor of Pseudomonas aeruginosa Deacetylase LpxC. Journal of medicinal chemistry. ISSN 1520-4804

Abstract

Over the past several decades the frequency of bacterial antimicrobial resistance in hospitals, including resistance to multiple antibacterials (multi-drug resistant, MDR) and its association with serious infectious diseases, have increased at alarming rates. Pseudomonas aeruginosa is a leading cause of nosocomial infections, and resistance to virtually all approved antibacterials is emerging in this pathogen. To address the need for new agents to treat MDR P. aeruginosa, we focused on inhibiting the first committed step in the biosynthesis of lipid A, the deacetylation of uridyldiphospho-3-O-(R-hydroxydecanoyl)-N-acetylglucosamine by the enzyme LpxC. We approached this through the design, synthesis and biological evaluation of several potent hydroxamic acid LpxC inhibitors, such as 1.

Item Type: Article
Date Deposited: 27 Jun 2017 00:45
Last Modified: 27 Jun 2017 00:45
URI: https://oak.novartis.com/id/eprint/31293

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