Coumarins effectively inhibit bacterial α-carbonic anhydrases.

ABSTRACT: Coumarins are known to act as prodrug inhibitors of mammalian α-carbonic anhydrases (CAs, EC 4.2.1.1) but they were not yet investigated for the inhibition of bacterial α-CAs. Here we demonstrate that such enzymes from the bacterial pathogens Neisseria gonorrhoeae (NgCAα) and Vibrio cholerae (VchCAα) are inhibited by a panel of simple coumarins incorporating hydroxyl, amino, ketone or carboxylic acid ester moieties in various positions of the ring system. The nature and the position of the substituents in the coumarin ring were the factors which strongly influenced inhibitory efficacy. NgCAα was inhibited with K_Is in the range of 28.6-469.5 µM, whereas VchCAα with K_Is in the range of 39.8-438.7 µM. The two human (h)CA isoforms included for comparison rea

SUBMITTER: Giovannuzzi S 

PROVIDER: S-EPMC8741243 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature