Samet Mert, Z. Alım, M. İşgör
Jun 11, 2015
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Journal
Arabian Journal of Chemistry
Abstract
Abstract In this study a series of pyrazole-3,4-dicarboxamide ( 3 – 10 ) derivatives bearing sulfonamide moiety were synthesized starting from 1-(3-nitrophenyl)-5-phenyl-1 H -pyrazole-3,4-dicarboxylic acid ( 1 ). The structures of synthesized molecules were characterized by FT-IR, 1 H NMR, 13 C NMR, and elemental analysis methods. Human carbonic anhydrase isoenzymes (hCA I and hCA II) were purified separately from erythrocyte cells by the Sepharose-4B-L-tyrosine-sulfanilamide affinity column chromatography and inhibitory effects of newly synthesized sulfonamides on esterase activities of these isoenzymes have been studied as in vitro . The K i values of compounds were found in the range of 0.056–110.400 μM for hCA I and 0.057–533.400 μM for hCA II. Compound 4 has the highest inhibitory effect for hCA I and hCA II while compound 5 showed lowest inhibition. The structure–activity relationships for the inhibition of these isoforms with the pyrazole-sulfonamides reported here were also elucidated.