info:eu-repo/semantics/article
Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability
Fecha
2014-02Registro en:
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
0002-7863
CONICET Digital
CONICET
Autor
O’Daniel, Peter I.
Peng, Zhihong
Pi, Hualiang
Testero, Sebastian Andres
Ding, Derong
Spink, Edward
Leemans, Erika J.
Boudreau, Marc A.
Yamaguchi, Takao
Schroeder, Valerie A
Wolter, William R.
Llarrull, Leticia Irene
Song, Wei
Lashtochkin, Elena
Shi, Qicun
Kumarasiri, Malika
Antunes, Nuno T.
Espahbodi, Mana
Lichtenwalter, Katerina
Suckow, Mark A.
Vakulenko, Sergei
Mobashery, Shahriar
Chang, Mayland
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.