Discovery of a new class of non-â-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity and oral bioavailability
; 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 Otros responsables
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02/2014
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American Chemical Society
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Journal of the American Chemical Society
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0002-7863
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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.
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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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