Approved Drugs Containing Thiols as Inhibitors of Metallo-β-lactamases: Strategy To Combat Multidrug-Resistant Bacteria
Journal of Medicinal Chemistry2015Vol. 58(8), pp. 3626–3630
Citations Over TimeTop 10% of 2015 papers
Franca‐Maria Klingler, Thomas A. Wichelhaus, Denia Frank, Jenifer Cuesta-Bernal, Jasmin El-Delik, H. Florian Müller, Hanno Sjuts, Stephan Göttig, Arno Koenigs, 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.
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