Repurposing FDA-approved sulphonamide carbonic anhydrase inhibitors for treatment of Neisseria gonorrhoeae.

ABSTRACT: Neisseria gonorrhoeae is a high-priority pathogen of concern due to the growing prevalence of resistance development against approved antibiotics. Herein, we report the anti-gonococcal activity of ethoxzolamide, the FDA-approved human carbonic anhydrase inhibitor. Ethoxzolamide displayed an MIC_50, against a panel of N. gonorrhoeae isolates, of 0.125 µg/mL, 16-fold more potent than acetazolamide, although both molecules exhibited almost similar potency against the gonococcal carbonic anhydrase enzyme (NgCA) in vitro. Acetazolamide displayed an inhibition constant (K_i) versus NgCA of 74 nM, while Ethoxzolamide^'s K_i was estimated to 94 nM. Therefore, the increased anti-gonococcal potency of ethoxzolamide was attrib

SUBMITTER: Abutaleb NS 

PROVIDER: S-EPMC8667909 | biostudies-literature | 2022 Dec

REPOSITORIES: biostudies-literature