Inhibitory effect of novel pyrazole carboxamide derivatives on human carbonic anhydrase enzyme

Şen E., Alim Z., Duran H., Işgör M. M., BEYDEMİR Ş., Kasimoʇullari R., ...Daha Fazla

Journal of Enzyme Inhibition and Medicinal Chemistry, cilt.28, sa.2, ss.328-336, 2013 (SCI-Expanded) identifier identifier

  • 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.