Potent inhibitors of LpxC for the treatment of Gram-negative infections.

Matthew F Brown, Usa Reilly, Joseph A Abramite, Joel T Arcari, Robert Oliver, Rose A Barham, Ye Che, Jinshan Michael Chen, Elizabeth M Collantes, Seung Won Chung, Charlene Desbonnet, Jonathan Doty, Matthew Doroski, Juntyma J Engtrakul, Thomas M Harris, Michael Huband, John D Knafels, Karen L Leach, Shenping Liu, Anthony Marfat, Andrea Marra, Eric McElroy, Michael Melnick, Carol A Menard, Justin I Montgomery, Lisa Mullins, Mark C Noe, John O'Donnell, Joseph Penzien, Mark S Plummer, Loren M Price, Veerabahu Shanmugasundaram, Christy Thoma, Daniel P Uccello, Joseph S Warmus, Donn G Wishka

Index: J. Med. Chem. 2nd ed., 55 , 914-923, (2012)

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Abstract

In this paper, we present the synthesis and SAR as well as selectivity, pharmacokinetic, and infection model data for representative analogues of a novel series of potent antibacterial LpxC inhibitors represented by hydroxamic acid.