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Pyridone methylsulfone hydroxamate LpxC inhibitors for the treatment of serious gram-negative infections.
Montgomery, Justin I; Brown, Matthew F; Reilly, Usa; Price, Loren M; Abramite, Joseph A; Arcari, Joel; Barham, Rose; Che, Ye; Chen, Jinshan Michael; Chung, Seung Won; Collantes, Elizabeth M; Desbonnet, Charlene; Doroski, Matthew; Doty, Jonathan; Engtrakul, Juntyma J; Harris, Thomas M; Huband, Michael; Knafels, John D; Leach, Karen L; Liu, Shenping; Marfat, Anthony; McAllister, Laura; McElroy, Eric; Menard, Carol A; Mitton-Fry, Mark; Mullins, Lisa; Noe, Mark C; O'Donnell, John; Oliver, Robert; Penzien, Joseph; Plummer, Mark; Shanmugasundaram, Veerabahu; Thoma, Christy; Tomaras, Andrew P; Uccello, Daniel P; Vaz, Alfin; Wishka, Donn G.
Affiliation
  • Montgomery JI; Worldwide Medicinal Chemistry, Pfizer Worldwide Research and Development, 445 Eastern Point Road, Groton, Connecticut 06340, United States. justin.montgomery@pfizer.com
J Med Chem ; 55(4): 1662-70, 2012 Feb 23.
Article in En | MEDLINE | ID: mdl-22257165
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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Full text: 1 Database: MEDLINE Therapeutic Methods and Therapies TCIM: Plantas_medicinales Main subject: Pyridones / Sulfonic Acids / Gram-Negative Bacterial Infections / Amidohydrolases / Gram-Negative Bacteria / Hydroxamic Acids / Anti-Bacterial Agents Language: En Journal: J Med Chem Year: 2012 Type: Article Affiliation country: United States
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Full text: 1 Database: MEDLINE Therapeutic Methods and Therapies TCIM: Plantas_medicinales Main subject: Pyridones / Sulfonic Acids / Gram-Negative Bacterial Infections / Amidohydrolases / Gram-Negative Bacteria / Hydroxamic Acids / Anti-Bacterial Agents Language: En Journal: J Med Chem Year: 2012 Type: Article Affiliation country: United States