10.6084/m9.figshare.2067999.v1 Erhan Başar Erhan Başar Ekrem Tunca Ekrem Tunca Metin Bülbül Metin Bülbül Muharrem Kaya Muharrem Kaya Synthesis of novel sulfonamides under mild conditions with effective inhibitory activity against the carbonic anhydrase isoforms I and II Taylor & Francis Group 2016 K i values LC 1 H NMR HRMS results show novel sulfonamides glaucoma treatment 13 C NMR inhibition effects FT-IR carbonic anhydrase isoenzymes carbonic anhydrase inhibitors aminobenzene sulfonamide affinity chromatography esterase activities carbonic anhydrase isoforms benzamide 4 compound II Novel sulfonamide derivatives 6 IC 50 sulfonyl chloride derivatives 5 2016-01-27 13:51:14 Journal contribution 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 <p>Novel sulfonamide derivatives <b>6a</b>–<b>i</b>, as new carbonic anhydrase inhibitors which candidate for glaucoma treatment, were synthesized from the reactions of 4-amino-<i>N</i>-(4-sulfamoylphenyl) benzamide <b>4</b> and sulfonyl chloride derivatives <b>5a</b>–<b>i</b> with high yield (71–90%). The structures of these compounds were confirmed by using spectral analysis (FT-IR, <sup>1</sup>H NMR, <sup>13</sup>C NMR, LC/MS and HRMS). The inhibition effects of <b>6a</b>–<b>i</b> 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-<i>p</i>-aminobenzene sulfonamide affinity chromatography, were studied as <i>in vitro</i>, and IC<sub>50</sub> and <i>K</i><sub>i</sub> values were determined. The results show that newly synthesized compounds have quite powerful inhibitory properties.</p>