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Design, Synthesis, and Properties of a Potent Inhibitor of Pseudomonas aeruginosa Deacetylase LpxC. 2017
Grazia Piizzi, and
David T Parker, and
Yunshan Peng, and
Markus Dobler, and
Anup Patnaik, and
Som Wattanasin, and
Eugene Liu, and
Francois Lenoir, and
Jill Nunez, and
John Kerrigan, and
David McKenney, and
Colin Osborne, and
Donghui Yu, and
Leanne Lanieri, and
Jade Bojkovic, and
JoAnn Dzink-Fox, and
Maria-Dawn Lilly, and
Elizabeth R Sprague, and
Yipin Lu, and
Hongming Wang, and
Srijan Ranjitkar, and
Lili Xie, and
Bing Wang, and
Meir Glick, and
Lawrence G Hamann, and
Ruben Tommasi, and
Xia Yang, and
Charles R Dean
Over the past several decades, the frequency of antibacterial resistance in hospitals, including multidrug resistance (MDR) and its association with serious infectious diseases, has increased at alarming rates. Pseudomonas aeruginosa is a leading cause of nosocomial infections, and resistance to virtually all approved antibacterial agents 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 novel hydroxamic acid LpxC inhibitors, exemplified by 1, where cytotoxicity against mammalian cell lines was reduced, solubility and plasma-protein binding were improved while retaining potent anti-pseudomonal activity in vitro and in vivo.
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