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J Am Chem Soc. 2014 Mar 5;136(9):3664-72. doi: 10.1021/ja500053x. Epub 2014 Feb 21.

Discovery of a new class of non-β-lactam inhibitors of penicillin-binding proteins with Gram-positive antibacterial activity.

Author information

1
Department of Chemistry and Biochemistry, University of Notre Dame , Notre Dame, Indiana 46556, United States.

Abstract

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.

PMID:
24517363
PMCID:
PMC3985699
DOI:
10.1021/ja500053x
[Indexed for MEDLINE]
Free PMC Article

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