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 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 31
  • Publication Date: 2016
  • Doi Number: 10.1080/14756366.2016.1198900
  • Journal Name: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.180-188
  • Keywords: Enzyme inhibition, gallic acid, p-hydroxybenzoic acid, MESSENGER-RNA EXPRESSION, ISOENZYMES I, ENZYME-ACTIVITY, CDNA CLONING, DRUG DESIGN, HCA I, DERIVATIVES, VITRO, VIVO, ANTIOXIDANT
  • Bezmialem Vakıf University Affiliated: No

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.