Synthesis and carbonic anhydrase inhibitory activities of new thienyl-substituted pyrazoline benzenesulfonamides

METE E., COMEZ B., GÜL H. İ., GÜLÇİN İ., SUPURAN C. T.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.31, ss.1-5, 2016 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 31
  • Basım Tarihi: 2016
  • Doi Numarası: 10.1080/14756366.2016.1181627
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.1-5
  • Anahtar Kelimeler: Benzenesulfonamides, carbonic anhydrase, pyrazoline, synthesis, thiophene, ANTIMICROBIAL AGENTS, ISOENZYMES I, ENZYME, DERIVATIVES, PATENT, ANTICANCER, ACTIVATORS, CHALCONES, SERIES
  • Atatürk Üniversitesi Adresli: Evet

Özet

A series of new thienyl-substituted pyrazoline benzenesulfonamides were synthesized and their carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activities were tested on the human (h) isoforms hCA I and hCA II. The inhibition constant (K-i) of these sulfonamides were in the range of 232.16-637.70nM toward the slow cytosolic isozyme hCA I, and in the range of 342.07-455.80nM toward hCA II. Many of these compounds showed comparable inhibition with the reference sulfonamide acetazolamide, a clinically used drug. As the sulfonamide CA inhibitors (CAIs) show many therapeutic uses, these derivatives represent interesting examples of a novel class of such derivatives.