Facile synthesis and characterization of novel pyrazole-sulfonamides and their inhibition effects on human carbonic anhydrase isoenzymes

Balseven H., Mustafa Işgör M., Mert S., Alim Z., BEYDEMİR Ş., Ok S., ...Daha Fazla

Bioorganic and Medicinal Chemistry, cilt.21, sa.1, ss.21-27, 2013 (SCI-Expanded) identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 21 Sayı: 1
  • Basım Tarihi: 2013
  • Doi Numarası: 10.1016/j.bmc.2012.11.012
  • Dergi Adı: Bioorganic and Medicinal Chemistry
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.21-27
  • Anahtar Kelimeler: Carbonic anhydrase, Diazonium, Inhibition, Pyrazole, Sulfonamide
  • Bilecik Şeyh Edebali Üniversitesi Adresli: Evet

Özet

In the current study, a series of pyrazole-sulfonamide derivatives (2-14) were synthesized, characterized, and the inhibition effects of the derivatives on human carbonic anhydrases (hCA I and hCA II) were investigated as in vitro. Structures of these sulfonamides were confirmed by FT-IR, 1H NMR, 13C NMR and LC-MS analysis. 1H NMR and 13C NMR revealed the tautomeric structures. hCA I and hCA II isozymes were purified from human erythrocytes and inhibitory effects of newly synthesized sulfonamides on esterase activities of these isoenzymes have been studied. The Ki values of compounds were 0.062-1.278 μM for hCA I and 0.012-0.379 μM for hCA II. The inhibition effects of 7 for hCA I and 4 for hCA II isozymes were almost in nanomolar concentration range. © 2012 Elsevier Ltd. All rights reserved.