| Literature DB >> 25815530 |
Franca-M Klingler, Thomas A Wichelhaus1, Denia Frank1, Jenifer Cuesta-Bernal, Jasmin El-Delik, H Florian Müller, Hanno Sjuts, Stephan Göttig1, Arno Koenigs1, Klaas M Pos, Denys Pogoryelov, Ewgenij Proschak.
Abstract
Resistance to β-lactam antibiotics can be mediated by metallo-β-lactamase enzymes (MBLs). An MBL inhibitor could restore the effectiveness of β-lactams. We report on the evaluation of approved thiol-containing drugs as inhibitors of NDM-1, VIM-1, and IMP-7. Drugs were assessed by a novel assay using a purchasable fluorescent substrate and thermal shift. Best compounds were tested in antimicrobial susceptibility assay. Using these orthogonal screening methods, we identified drugs that restored the activity of imipenem.Entities:
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Year: 2015 PMID： 25815530 DOI： 10.1021/jm501844d
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446