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Bioorg Med Chem Lett. 2012 Oct 1;22(19):6229-32. doi: 10.1016/j.bmcl.2012.08.012. Epub 2012 Aug 10.

2-Substituted 4,5-dihydrothiazole-4-carboxylic acids are novel inhibitors of metallo-β-lactamases.

Author information

1
Department of Pharmacology, Baylor College of Medicine, 1 Baylor Plaza, Houston, TX 77030, United States.

Abstract

Bacterial resistance to β-lactam antibiotics caused by class B metallo-β-lactamases (MBL), especially for certain hospital-acquired, Gram-negative pathogens, poses a significant threat to public health. We report several 2-substituted 4,5-dihydrothiazole-4-carboxylic acids to be novel MBL inhibitors. Structure activity relationship (SAR) and molecular modeling studies were performed and implications for further inhibitor design are discussed.

PMID:
22921080
PMCID:
PMC3463135
DOI:
10.1016/j.bmcl.2012.08.012
[Indexed for MEDLINE]
Free PMC Article

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