1136832-72-8Relevant articles and documents
Discovery of a new class of non-β-lactam inhibitors of penicillin-binding proteins with gram-positive antibacterial activity
O'Daniel, Peter I.,Peng, Zhihong,Pi, Hualiang,Testero, Sebastian A.,Ding, Derong,Spink, Edward,Leemans, Erika,Boudreau, Marc A.,Yamaguchi, Takao,Schroeder, Valerie A.,Wolter, William R.,Llarrull, Leticia I.,Song, Wei,Lastochkin, Elena,Kumarasiri, Malika,Antunes, Nuno T.,Espahbodi, Mana,Lichtenwalter, Katerina,Suckow, Mark A.,Vakulenko, Sergei,Mobashery, Shahriar,Chang, Mayland
, p. 3664 - 3672 (2014/03/21)
Infections caused by hard-to-treat methicillin-resistant Staphylococcus aureus (MRSA) are a serious global public-health concern, as MRSA has become broadly resistant to many classes of antibiotics. We disclose herein the discovery of a new class of non-β-lactam antibiotics, the oxadiazoles, which inhibit penicillin-binding protein 2a (PBP2a) of MRSA. The oxadiazoles show bactericidal activity against vancomycin-and linezolid-resistant MRSA and other Gram-positive bacterial strains, in vivo efficacy in a mouse model of infection, and have 100% oral bioavailability.
ANTIBACTERIAL COMPOUNDS AND METHODS OF USING SAME
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Page/Page column 11-12; Sheet 2, (2009/05/29)
Embodiments of the present invention provide novel antibactehals that target penicillin-binding proteins or other important cellular targets. Methods for inhibiting growth (reproduction, etc.) of bacteria using compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, such as certain strains of Entercoccus and Staphylococcus aureus.