1. Structure-activity relationships of biphenyl tetrazoles as metallo-β-lactamase inhibitors
- Author
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Gail G. Hammond, Walter J. May, Steven M. Hutchins, Jeffrey H. Toney, Wallace T. Ashton, Xiling Yuan, Dana E. Vanderwall, and Kelly A. Cleary
- Subjects
medicine.drug_class ,Stereochemistry ,Clinical Biochemistry ,Antibiotics ,Tetrazoles ,Pharmaceutical Science ,Biochemistry ,Bacteroides fragilis ,Structure-Activity Relationship ,Drug Discovery ,polycyclic compounds ,medicine ,Structure–activity relationship ,Enzyme Inhibitors ,Molecular Biology ,Antibacterial agent ,chemistry.chemical_classification ,biology ,Chemistry ,Organic Chemistry ,biochemical phenomena, metabolism, and nutrition ,bacterial infections and mycoses ,biology.organism_classification ,Enzyme ,Enzyme inhibitor ,biology.protein ,bacteria ,Molecular Medicine ,beta-Lactamase Inhibitors ,Bacteria ,Pseudomonadaceae ,Membrane dipeptidase - Abstract
Resistance to carbapenem antibiotics in gram-negative bacteria is due, in part, to expression of a wide spectrum metallo-beta-lactamase, which renders the drug inactive. Biphenyl tetrazoles containing 3-n-butyl-1-phenylpyrazole-5-carboxylates or the corresponding 5-ethyl esters were found to inhibit metallo-beta-lactamases as well as renal dehydropeptidase I to a lesser extent.
- Published
- 1999
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