Facile synthesis and characterization of novel pyrazole-sulfonamides and their inhibition effects on human carbonic anhydrase isoenzymes
Bioorganic and Medicinal Chemistry, vol.21, no.1, pp.21-27, 2013 (SCI-Expanded, Scopus)
- Publication Type: Article / Article
- Volume: 21 Issue: 1
- Publication Date: 2013
- Doi Number: 10.1016/j.bmc.2012.11.012
- Journal Name: Bioorganic and Medicinal Chemistry
- Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Page Numbers: pp.21-27
- Keywords: Carbonic anhydrase, Diazonium, Inhibition, Pyrazole, Sulfonamide
- Bilecik Şeyh Edebali University Affiliated: Yes
Abstract
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.