Optimized Ebselen-Based Inhibitors of Bacterial Ureases with Nontypical Mode of Action

Optimized Ebselen-Based Inhibitors of Bacterial Ureases with Nontypical Mode of Action

Screening of 25 analogs of Ebselen, diversified at the N-aromatic residue, led to the identification of the most potent inhibitors of Sporosarcina pasteurii urease reported to date. The presence of a dihalogenated phenyl ring caused exceptional activity of these 1,2-benzisoselenazol-3­(2H)-ones, wit...

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Veröffentlicht in:Journal of medicinal chemistry 2023-02, Vol.66 (3), p.2054-2063
Hauptverfasser: Macegoniuk, Katarzyna, Tabor, Wojciech, Mazzei, Luca, Cianci, Michele, Giurg, Mirosław, Olech, Kamila, Burda-Grabowska, Małgorzata, Kaleta, Rafał, Grabowiecka, Agnieszka, Mucha, Artur, Ciurli, Stefano, Berlicki, Łukasz
Format: Artikel
Sprache:eng
Schlagworte:
Azoles - pharmacology
Bacteria - metabolism
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Isoindoles - pharmacology
Urease
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Zusammenfassung:Screening of 25 analogs of Ebselen, diversified at the N-aromatic residue, led to the identification of the most potent inhibitors of Sporosarcina pasteurii urease reported to date. The presence of a dihalogenated phenyl ring caused exceptional activity of these 1,2-benzisoselenazol-3­(2H)-ones, with Ki value in a low picomolar range (
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.2c01799