Synthesis, characterization and biological evaluation of pyrazole-based benzene sulfonamides as inhibitors of human carbonic anhydrase II, IX and XII.

ABSTRACT: The aberrant level of the carbonic anhydrase isozymes is linked with various disorders which include glaucoma, epilepsy, altitude sickness and obesity. In the present study, a series of the pyrazole-based benzene sulfonamides derivatives (4a-4l) were designed, synthesized and evaluated as the inhibitors of the three isoforms of human carbonic anhydrases (hCAII, hCAIX and hCAXII). A number of the derivatives were found more active inhibitors than acetazolamide used as a standard against the human hCAII, hCAIX and hCAXII. Among the series, the compound 4k inhibited the hCAII to a submicromolar level presenting the IC₅₀ ± SEM concentration of 0.24 ± 0.18 μM, the inhibitor 4j reduced the activity of the hCAIX to the IC₅₀ ± SEM equals 0.15 ± 0.07 μM, whereas, the molecule

SUBMITTER: Hussain T 

PROVIDER: S-EPMC10280043 | biostudies-literature | 2023 Jun

REPOSITORIES: biostudies-literature