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>