1567711-31-2Relevant academic research and scientific papers
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.
