Artículo

Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability

O’Daniel, Peter I.; Peng, Zhihong; Pi, Hualiang; Testero, Sebastian AndresIcon ; Ding, Derong; Spink, Edward; Leemans, Erika J.; Boudreau, Marc A.; Yamaguchi, Takao; Schroeder, Valerie A; Wolter, William R.; Llarrull, Leticia IreneIcon ; Song, Wei; Lashtochkin, Elena; Shi, Qicun; Kumarasiri, Malika; Antunes, Nuno T.; Espahbodi, Mana; Lichtenwalter, Katerina; Suckow, Mark A.; Vakulenko, Sergei; Mobashery, Shahriar; Chang, Mayland
Fecha de publicación: 02/2014
Editorial: American Chemical Society
Revista: Journal of the American Chemical Society
ISSN: 0002-7863
Idioma: Inglés
Tipo de recurso: Artículo publicado
Clasificación temática:

Resumen

Infections caused by hard-to-treat methicillin-resistantStaphylococcus aureus(MRSA) are a serious global public-health concern,as MRSA has become broadly resistant to many classes of antibiotics. Wedisclose herein the discovery of a new class of non-β-lactam antibiotics,the oxadiazoles, which inhibit penicillin-binding protein 2a (PBP2a) ofMRSA. The oxadiazoles show bactericidal activity against vancomycin-and linezolid-resistant MRSA and other Gram-positive bacterial strains,invivoefficacy in a mouse model of infection, and have 100% oralbioavailability.
Palabras clave: Antibiotics , Mrsa , Oxadiazoles , Penicillin Binding Proteins
 
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info:eu-repo/semantics/openAccess Excepto donde se diga explícitamente, este item se publica bajo la siguiente descripción: Creative Commons Attribution-NonCommercial-ShareAlike 2.5 Unported (CC BY-NC-SA 2.5)
Identificadores
URI: http://hdl.handle.net/11336/31218
DOI: http://dx.doi.org/10.1021/ja500053x
URL: http://pubs.acs.org/doi/10.1021/ja500053x
Colecciones
Articulos(IBR)
Articulos de INST.DE BIOLOGIA MOLECULAR Y CELULAR DE ROSARIO
Articulos(IQUIR)
Articulos de INST.DE QUIMICA ROSARIO
Citación
O’Daniel, Peter I.; Peng, Zhihong; Pi, Hualiang; Testero, Sebastian Andres; Ding, Derong; et al.; Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability; American Chemical Society; Journal of the American Chemical Society; 136; 2-2014; 3664-3672
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