Pyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious gram-negative infections.

Autor: Montgomery JI; Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, 445 Eastern Point Road, Groton, Connecticut 06340, United States. justin.montgomery@pfizer.com, Brown MF, Reilly U, Price LM, Abramite JA, Arcari J, Barham R, Che Y, Chen JM, Chung SW, Collantes EM, Desbonnet C, Doroski M, Doty J, Engtrakul JJ, Harris TM, Huband M, Knafels JD, Leach KL, Liu S, Marfat A, McAllister L, McElroy E, Menard CA, Mitton-Fry M, Mullins L, Noe MC, O'Donnell J, Oliver R, Penzien J, Plummer M, Shanmugasundaram V, Thoma C, Tomaras AP, Uccello DP, Vaz A, Wishka DG
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 2012 Feb 23; Vol. 55 (4), pp. 1662-70. Date of Electronic Publication: 2012 Feb 08.
DOI: 10.1021/jm2014875
Abstrakt: 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.
Databáze: MEDLINE