Inhibitory effect of novel pyrazole carboxamide derivatives on human carbonic anhydrase enzyme
Journal of Enzyme Inhibition and Medicinal Chemistry, cilt.28, sa.2, ss.328-336, 2013 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 28 Sayı: 2
- Basım Tarihi: 2013
- Doi Numarası: 10.3109/14756366.2011.651465
- Dergi Adı: Journal of Enzyme Inhibition and Medicinal Chemistry
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
- Sayfa Sayıları: ss.328-336
- Anahtar Kelimeler: Antiglaucoma, Hydrogen bonding, Inhibition effect, Pyrazole-3-carboxamide, Tautomeric structures
- Bilecik Şeyh Edebali Üniversitesi Adresli: Evet
Özet
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.