Potent Inhibitors of LpxC for the Treatment of Gram-Negative Infections

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• 作者：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鈥橠onnell ; Joseph Penzien ; Mark S. Plummer ; Loren M. Price ; Veerabahu Shanmugasundaram ; Christy Thoma ; Daniel P. Uccello ; Joseph S. Warmus ; Donn G. Wishka
• 刊名：Journal of Medicinal Chemistry
• 出版年：2012
• 出版时间：January 26, 2012
• 年：2012
• 卷：55
• 期：2
• 页码：914-923
• 全文大小：480K
• 年卷期：v.55,no.2(January 26, 2012)
• ISSN：1520-4804

文摘

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 1a.