Department of Chemistry, Art and Science Faculty, Dumlupinar University, Kutahya, Turkey.
J Enzyme Inhib Med Chem. 2013 Apr;28(2):311-5. doi: 10.3109/14756366.2012.712516. Epub 2012 Sep 7.
Three novel metal complexes of N-[5-(aminosulfonyl)-1,3,4-thiadiazol-2-yl]-4-benzoyl-1-(3-nitrophenyl)-5-phenyl-1H-pyrazole-3-carboxamide which possess strong carbonic anhydrase (CA) inhibitory properties have been synthesised. The structure of these compounds has been investigated by elemental analysis, FT-IR, LC/MS, UV-vis spectrophotometric method and magnetic susceptibility. Human carbonic anhydrase isoenzymes hCA-I and hCA-II were purified from erythrocyte cells by the affinity chromatography. The inhibitory effects of newly synthesized complexes and acetazolamide (AAZ) as a control compound on hydratase and esterase activities of these isoenzymes have been studied in vitro by comparing IC(50) and K(i) values and it has been found that the newly synthesised complexes behave as very powerful inhibitors against hCA-I and hCA-II than parent ligand (1) and than AAZ.
已经合成了三种新型的 N-[5-(氨磺酰基)-1,3,4-噻二唑-2-基]-4-苯甲酰基-1-(3-硝基苯基)-5-苯基-1H-吡唑-3-甲酰胺的金属配合物，它们具有很强的碳酸酐酶（CA）抑制特性。通过元素分析、FT-IR、LC/MS、UV-vis 分光光度法和磁化率对这些化合物的结构进行了研究。人碳酸酐酶同工酶 hCA-I 和 hCA-II 从红细胞细胞中通过亲和层析进行纯化。通过比较 IC50 和 K(i) 值，研究了新合成的配合物和乙酰唑胺（AAZ）作为对照化合物对这些同工酶的水合酶和酯酶活性的抑制作用，结果发现新合成的配合物对 hCA-I 和 hCA-II 的抑制作用比母体配体（1）和 AAZ 更强。
