期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 136, 期 9, 页码 3664-3672出版社
AMER CHEMICAL SOC
DOI: 10.1021/ja500053x
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资金
- National Institutes of Health [AI090818]
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-beta-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.
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