Pyridone Methylsulfone Hydroxamate LpxC Inhibitors for the Treatment of Serious Gram-Negative Infections
Journal of Medicinal Chemistry2012Vol. 55(4), pp. 1662–1670
Citations Over TimeTop 12% of 2012 papers
Justin I. Montgomery, Matthew F. Brown, Usa Reilly, Loren Price, J. A. Abramite, Joel T. Arcari, Rose A. Barham, Ye Che, Jinshan Michael Chen, Seung Won Chung, Elizabeth M. Collantes, Charlene Desbonnet, Matthew Doroski, Jonathan L. Doty, Juntyma J. Engtrakul, Thomas M. Harris, Michael D. Huband, John D. Knafels, Karen L. Leach, Shenping Liu, Anthony Marfat, Laura A. McAllister, Eric B. McElroy, Carol A. Menard, Mark J. Mitton‐Fry, Lisa Mullins, Mark C. Noe, John P. O’Donnell, Robert M. Oliver, Joseph Penzien, Mark S. Plummer, Veerabahu Shanmugasundaram, Christy L. Thoma, Andrew P. Tomaras, Daniel P. Uccello, Alfin D. N. Vaz, Donn G. Wishka
Abstract
The synthesis and biological activity of a new series of LpxC inhibitors represented by pyridone methylsulfone hydroxamate 2a 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.
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