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  • Nitroxoline and its derivatives are potent inhibitors of metallo-▫$\beta$▫-lactamases
    Proschak, Anna ...
    Carbapenemases such as metallo-[beta]-lactamases (MBLs) are spreading among Gram-negative bacterial pathogens. Infections due to these multidrug-resistant bacteria constitute a major global health ... challenge. Therapeutic strategies against carbapenemase producing bacteria include [beta]-lactamase inhibitor combinations. Nitroxoline is a broad-spectrum antibiotic with restricted indication for urinary tract infections. In this study, we report on nitroxoline as an inhibitor of MBLs. We investigate the structure-activity relationships of nitroxoline derivatives considering in vitro MBL inhibitory potency in a fluorescence based assay using purified recombinant MBLs, NDM-1 and VIM-1. We investigated the most potent nitroxoline derivative in combination with imipenem against clinical isolates as well as transformants producing MBL by broth microdilution and time-kill kinetics. Our findings demonstrate that nitroxoline derivatives are potent MBL inhibitors and in combination with imipenem overcome MBL-mediated carbapenem resistance.
    Source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 228, 2022, str. 1-10)
    Type of material - article, component part ; adult, serious
    Publish date - 2022
    Language - english
    COBISS.SI-ID - 84869891

    Link(s):

    https://www.sciencedirect.com/science/article/pii/S0223523421008242#!
    DOI

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