Synthesis and carbonic anhydrase inhibitory activities of new thienyl-substituted pyrazoline benzenesulfonamides
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.31, ss.1-5, 2016 (SCI-Expanded, Scopus)
- 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.