A class of sulfonamides as carbonic anhydrase I and II inhibitors


Gokcen T., GÜLÇİN İ., Ozturk T. , GOREN A. C.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.31, pp.180-188, 2016 (Journal Indexed in SCI) identifier identifier

  • Publication Type: Article / Article
  • Volume: 31
  • Publication Date: 2016
  • Doi Number: 10.1080/14756366.2016.1198900
  • Title of Journal : JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Page Numbers: pp.180-188

Abstract

Four groups of novel sulfonamide derivatives: (i) acetoxybenzamide, (ii) triacetoxybenzamide, (iii) hydroxybenzamide and (iv) trihydroxybenzamide, all having thiazole, pyrimidine, pyridine, isoxazole and thiadiazole moieties were prepared and their inhibitory effects were studied on two metalloenzymes, i.e. carbonic anhydrase isozymes (hCA I and II), purified from human erythrocyte cells by Sepharose-4B-l-tyrosine-sulfanilamide affinity chromatography. These enzymes are present in almost all living organisms to catalyse the synthesis of bicarbonate ion (HCO3-) from carbon dioxide and water. The sulfonamide derivatives were found to be active against hCA I and II in the range of 2.62-136.54 and 5.74-210.58nM, respectively.