Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 22, Issue 19, Pages 6229-6232Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.08.012
Keywords
Metallo-beta-lactamase; Inhibitor; Rational design; Molecular modeling
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Funding
- National Institute of Allergy and Infectious Disease (NIAID/NIH) [R21AI090190]
- NIAID/NIH [R01AI32956]
- NIH/NIDDK [T90DK070109]
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Bacterial resistance to beta-lactam antibiotics caused by class B metallo-beta-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. (C) 2012 Elsevier Ltd. All rights reserved.
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