Pyridone Methylsulfone Hydroxamate LpxC Inhibitors for the Treatment of Serious Gram-Negative Infections
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- 作者：Justin I. Montgomery ; Matthew F. Brown ; Usa Reilly ; Loren M. Price ; Joseph A. Abramite ; Joel Arcari ; Rose Barham ; Ye Che ; Jinshan Michael Chen ; Seung Won Chung ; Elizabeth M. Collantes ; Charlene Desbonnet ; Matthew Doroski ; Jonathan Doty ; Juntyma J. Engtrakul ; Thomas M. Harris ; Michael Huband ; John D. Knafels ; Karen L. Leach ; Shenping Liu ; Anthony Marfat ; Laura McAllister ; Eric McElroy ; Carol A. Menard ; Mark Mitton-Fry ; Lisa Mullins ; Mark C. Noe ; John O鈥橠onnell ; Robert Oliver ; Joseph Penzien ; Mark Plummer ; Veerabahu Shanmugasundaram ; Christy Thoma ; Andrew P. Tomaras ; Daniel P. Uccello ; Alfin Vaz ; Donn G. Wishka
- 刊名：Journal of Medicinal Chemistry
- 出版年：2012
- 出版时间：February 23, 2012
- 年：2012
- 卷：55
- 期：4
- 页码：1662-1670
- 全文大小：440K
- 年卷期：v.55,no.4(February 23, 2012)
- ISSN：1520-4804
文摘
The synthesis and biological activity of a new series of LpxC inhibitors represented by pyridone methylsulfone hydroxamate <b>2ab> is presented. Members of this series have improved solubility and free fraction when compared to compounds in the previously described biphenyl methylsulfone hydroxamate series, and they maintain superior Gram-negative antibacterial activity to comparator agents.