Faculty of Art and Science, Department of Chemistry, Dumlupinar University, Kutahya, Turkey.
J Enzyme Inhib Med Chem. 2013 Apr;28(2):328-36. doi: 10.3109/14756366.2011.651465. Epub 2012 Feb 3.
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.
本文介绍了新型吡唑甲酰胺衍生物（2-9）的合成、表征和生物评价。（1）H 和（13）C NMR 用于结构描述、可能的互变异构结构确定和氢键观察。FT-IR 结果证实了吡唑衍生物的合成，而热重分析证实了热稳定性高达 300°C。熔点强烈依赖于它们的晶体结构，这一点通过差示扫描量热法和 X 射线衍射测量得到了证实。通过体外从人红细胞中纯化的碳酸酐酶 I 和 II（CA-I 和 II）同工酶研究了 2-9 作为潜在抗青光眼药物的影响。化合物 3 和 9 具有最高的抑制作用，而化合物 6 和 8 显示出最低的抑制作用。
