%0 Journal Article %A Başar, Erhan %A Tunca, Ekrem %A Bülbül, Metin %A Kaya, Muharrem %D 2016 %T Synthesis of novel sulfonamides under mild conditions with effective inhibitory activity against the carbonic anhydrase isoforms I and II %U https://tandf.figshare.com/articles/journal_contribution/Synthesis_of_novel_sulfonamides_under_mild_conditions_with_effective_inhibitory_activity_against_the_carbonic_anhydrase_isoforms_I_and_II/2067999 %R 10.6084/m9.figshare.2067999.v1 %2 https://ndownloader.figshare.com/files/3685905 %K K i values %K LC %K 1 H NMR %K HRMS %K results show %K novel sulfonamides %K glaucoma treatment %K 13 C NMR %K inhibition effects %K FT-IR %K carbonic anhydrase isoenzymes %K carbonic anhydrase inhibitors %K aminobenzene sulfonamide affinity chromatography %K esterase activities %K carbonic anhydrase isoforms %K benzamide 4 %K compound %K II Novel sulfonamide derivatives 6 %K IC 50 %K sulfonyl chloride derivatives 5 %X

Novel sulfonamide derivatives 6ai, as new carbonic anhydrase inhibitors which candidate for glaucoma treatment, were synthesized from the reactions of 4-amino-N-(4-sulfamoylphenyl) benzamide 4 and sulfonyl chloride derivatives 5ai with high yield (71–90%). The structures of these compounds were confirmed by using spectral analysis (FT-IR, 1H NMR, 13C NMR, LC/MS and HRMS). The inhibition effects of 6ai on the hydratase and esterase activities of human carbonic anhydrase isoenzymes, hCA I and II, which were purified from human erythrocytes with Sepharose®4B-l-tyrosine-p-aminobenzene sulfonamide affinity chromatography, were studied as in vitro, and IC50 and Ki values were determined. The results show that newly synthesized compounds have quite powerful inhibitory properties.

%I Taylor & Francis