Inhibitory effect of novel pyrazole carboxamide derivatives on human carbonic anhydrase enzyme.
The synthesis, characterization and biological evaluation of novel pyrazole carboxamide derivatives (2-9) are presented. (1)H and (13)C 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.
Faculty of Art and Science, Department of Chemistry, Dumlupinar University, Kutahya, Turkey.
Elvan
E
Şen
Zuhal
Z
Alim
Hatice
H
Duran
Mehmet Mustafa
MM
İşgör
Şükrü
Ş
Beydemir
Rahmi
R
Kasimoğullari
Salim
S
Ok
D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000302:isolation & purification / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D004912:Erythrocytes / Q000201:enzymology; D006801:Humans; D015394:Molecular Structure; D020033:Protein Isoforms / Q000037:antagonists & inhibitors / Q000302:isolation & purification / Q000378:metabolism; D011720:Pyrazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D002257:Carbonic Anhydrase Inhibitors; D020033:Protein Isoforms; D011720:Pyrazoles; D002256:Carbonic Anhydrases