Inhibitory effect of novel pyrazole carboxamide derivatives on human carbonic anhydrase enzyme
Journal of Enzyme Inhibition and Medicinal Chemistry, vol.28, no.2, pp.328-336, 2013 (SCI-Expanded, Scopus)
- Publication Type: Article / Article
- Volume: 28 Issue: 2
- Publication Date: 2013
- Doi Number: 10.3109/14756366.2011.651465
- Journal Name: Journal of Enzyme Inhibition and Medicinal Chemistry
- Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Page Numbers: pp.328-336
- Keywords: Antiglaucoma, Hydrogen bonding, Inhibition effect, Pyrazole-3-carboxamide, Tautomeric structures
- Bilecik Şeyh Edebali University Affiliated: Yes
Abstract
The synthesis, characterization and biological evaluation of novel pyrazole carboxamide derivatives (2-9) are presented. H and 13C NMR have been used for the structure description, possible tautomeric structures determination and hydrogen bonding observation. FT-IR results have confirmed the synthesis of the pyrazole derivatives while thermal gravimetric analysis has confirmed thermal stability up to 300°C. The melting temperatures are strongly dependent on their crystal structure as confirmed by differential scanning calorimetry and X-ray diffraction measurements. Impacts of 2-9 as possible antiglaucoma agents were investigated on carbonic anhydrase I and II (CA-I and II) isozymes purified from human erythrocytes in vitro. Compounds 3 and 9 had the highest inhibitory effect while compounds 6 and 8 showed the lowest inhibition.