Inhibition studies of bacterial α-carbonic anhydrases with phenols.

ABSTRACT: The α-class carbonic anhydrases (CAs, EC 4.2.1.1) from the bacterial pathogens Neisseria gonorrhoeae (NgCAα) and Vibrio cholerae (VchCAα) were investigated for their inhibition by a panel of phenols and phenolic acids. Mono-, di- and tri-substituted phenols incorporating additional hydroxyl/hydroxymethyl, amino, acetamido, carboxyl, halogeno and carboxyethenyl moieties were included in the study. The best NgCAα inhibitrs were phenol, 3-aminophenol, 4-hydroxy-benzylalcohol, 3-amino-4-chlorophenol and paracetamol, with K_I values of 0.6-1.7 µM. The most effective VchCAα inhibitrs were phenol, 3-amino-4-chlorophenol and 4-hydroxy-benzyl-alcohol, with K_I values of 0.7-1.2 µM. Small changes in the phenol scaffold led to drastic effects on the bacterial CA inhi

SUBMITTER: Giovannuzzi S 

PROVIDER: S-EPMC8843131 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature