Discovery of a new class of non-ß-lactam inhibitors of penicillin-binding proteins with gram-positive antibacterial activity
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Date
2014
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O'Daniel, P.I.
Peng, Z.
Pi, H.
Testero, S.A.
Kumarasiri, M.
Chang, M.
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Journal of the American Chemical Society, 2014; 136(9):3664-3672
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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 vancomycinand linezolid-resistant MRSA and other Gram-positive bacterial strains, in vivo efficacy in a mouse model of infection, and have 100% oral bioavailability.
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Copyright 2014 American Chemical Society