Erzurum Technical University Erzurum

Erzurum, Turkey

Erzurum Technical University Erzurum

Erzurum, Turkey
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Akbaba Y.,Erzurum Technical University Erzurum | Akbaba Y.,Gumushane University | Bastem E.,Gumushane University | Topal F.,Gumushane University | And 6 more authors.
Archiv der Pharmazie | Year: 2014

Three 1-aminoindanes, four anilines and BnOH or t-BuOH were reacted with chlorosulfonyl isocyanate to give sulfamoyl carbamates. Pd-C catalysed hydrogenolysis reactions of carbamates or deprotection of the Boc group of the carbamates with CF3CO2H afforded seven novel sulfamides. Human carbonic anhydrase (hCA) isoenzymes I and II (hCA I and hCA II) were purified from fresh human blood erythrocytes with onestep affinity chromatography on Sepharose 4B-tyrosine-sulfanilamide. The inhibitory properties of the novel sulfamides on both isoenzymes were determined using the esterase activity with 4-nitrophenyl acetate (NPA) as substrate. The tested novel sulfamides derived from 1-aminoindanes and anilines effectively inhibited hCA I and II competitively in the nanomolar range. Among these compounds, the novel sulfamide derivative 17 showed themost potent inhibitory effect against hCA I (Ki: 153.88 nM), while sulfamide derivative 26 showed the highest inhibitory potential against hCA II (Ki: 117.80nM). © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.

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