Pyridine-2,6-Dithiocarboxylic Acid and Its Metal Complexes: New Inhibitors of New Delhi Metallo -Lactamase-1

Autor: Chris S. Thomas, Doug R. Braun, Jose Luis Olmos, Scott R. Rajski, George N. Phillips, David N. Andes, Tim S. Bugni
Jazyk: angličtina
Rok vydání: 2020
Předmět:
Zdroj: Marine Drugs, Vol 18, Iss 6, p 295 (2020)
Druh dokumentu: article
ISSN: 1660-3397
DOI: 10.3390/md18060295
Popis: Carbapenem-resistant Enterobacteriaceae continue to threaten human health worldwide with few effective treatment options. New Delhi metallo--lactamase (NDM) enzymes are a contributing element that drive resistance to many -lactam- and carbapenem-based antimicrobials. Many NDM inhibitors are known, yet none are clinically viable. In this study, we present and characterize a new class of NDM-1 inhibitors based on a pyridine-2,6-dithiocarboxylic acid metal complex scaffold. These complexes display varied and unique activity profiles against NDM-1 in kinetic assays and serve to increase the effectiveness of meropenem, an established antibacterial, in assays using clinical Enterobacteriaceae isolates.
Databáze: Directory of Open Access Journals