Exploration of Thiourea-Based Scaffolds for the Construction of Bacterial Ureases Inhibitors.

ABSTRACT: A series of 32 thiourea-based urease inhibitors were synthesized and evaluated against native bacterial enzyme and whole cells of Sporosarcina pasteurii and Proteus mirabilis strains. The proposed inhibitors represented structurally diverse thiosemicarbazones and thiocarbohydrazones, benzyl-substituted thiazolyl thioureas, 1H-pyrazole-1-carbothioamides, and dihydropirimidine-2(1H)-thiones. Kinetic characteristics with purified S. pasteurii enzyme determined low micromolar inhibitors within each structural group. (E)-2-(1-Phenylethylidene)hydrazine-1-carbothioamide 19 (K_i = 0.39 ± 0.01 μM), (E)-2-(4-methylbenzylidene)hydrazine-1-carbothioamide 16 (K_i = 0.99 ± 0.04 μM), and N</

SUBMITTER: Tabor W 

PROVIDER: S-EPMC10413841 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature