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Nitroxoline and its derivatives are potent inhibitors of metallo-▫$\beta$▫-lactamasesProschak, 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, seriousPublish date - 2022Language - englishCOBISS.SI-ID - 84869891
Author
Proschak, Anna |
Martinelli, Giada |
Frank, Denia |
Rotter J., Marco |
Brunst, Steffen |
Weizel, Lilia |
Burgers D., Luisa |
Fürst, Robert |
Proschak, Ewgenij |
Sosič, Izidor |
Gobec, Stanislav, 1970-
Topics
Bakterijska rezistenca |
Farmacevtska kemija |
kovinski kelatorji |
nitroksolin |
odpornost na bakterije |
metallo-[beta]-lactamases |
antibiotic resistance |
nitroxoline |
metal chelators
Author | Proschak, Anna ... |
Title | Nitroxoline and its derivatives are potent inhibitors of metallo-▫$\beta$▫-lactamases |
Publication date | 2022-01-15 |
COBISS.SI-ID | 84869891 |
Publication version in repository | Publisher's version |
Publication licence | Creative Commons Attribution 4.0 International |
Embargo | Immediate publication for public |
Project(s) from which the publication was funded
Title | Acronym | Project ID | Funder |
---|---|---|---|
Farmacevtska kemija: načrtovanje, sinteza in vrednotenje učinkovin | P1-0208-2015 |
Javna agencija za znanstvenoraziskovalno in inovacijsko dejavnost Republike Slovenije |
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https://www.sciencedirect.com/science/article/pii/S0223523421008242#! |
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Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Proschak, Anna | |
Martinelli, Giada | |
Frank, Denia | |
Rotter J., Marco | |
Brunst, Steffen | |
Weizel, Lilia | |
Burgers D., Luisa | |
Fürst, Robert | |
Proschak, Ewgenij | |
Sosič, Izidor | 30816 |
Gobec, Stanislav, 1970- | 15284 |
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