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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.
Afiliação
  • 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 em 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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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piridonas / Ácidos Sulfônicos / Infecções por Bactérias Gram-Negativas / Amidoidrolases / Bactérias Gram-Negativas / Ácidos Hidroxâmicos / Antibacterianos Limite: Animals / Humans Idioma: En Revista: J Med Chem Ano de publicação: 2012 Tipo de documento: Article
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Piridonas / Ácidos Sulfônicos / Infecções por Bactérias Gram-Negativas / Amidoidrolases / Bactérias Gram-Negativas / Ácidos Hidroxâmicos / Antibacterianos Limite: Animals / Humans Idioma: En Revista: J Med Chem Ano de publicação: 2012 Tipo de documento: Article