Department of Food Technology, Çanakkale 18 Mart University, Çanakakale, Turkey.
Department of Chemistry, Faculty of Art and Sciences, Sakarya University, Sakarya, Turkey.
J Biochem Mol Toxicol. 2020 Dec;34(12):e22596. doi: 10.1002/jbt.22596. Epub 2020 Aug 6.
Human carbonic anhydrase I and II isoenzymes (hCA I and II) are important metabolic enzymes. In this study, a new series of thiazol-(2(3H)-ylideneamino)benzenesulfonamide derivatives were synthesized and also some inhibition parameters including IC (hydratese) and inhibition constant values (K , esterase) were determined. All studied compounds exhibited potent inhibition against these enzymes. They inhibited carbonic anhydrases (CAs) with the IC values of 113 to 395.8 nM (K = 77.38-319.59 nM) for hCA I and 91.9 to 516 nM (K = 62.79-425.89 nM) for hCA II. Among the compounds, 5c was found to be the most active one (K : 77.38 nM) for hCA I and 5g was found for hCA II with the value of 62.79 nM.
人碳酸酐酶 I 和 II 同工酶（hCA I 和 II）是重要的代谢酶。在这项研究中，合成了一系列新的噻唑-（2（3H）-亚基）苯磺酰胺衍生物，并测定了一些抑制参数，包括 IC（hydratese）和抑制常数值（K ，酯酶）。所有研究的化合物都表现出对这些酶的强抑制作用。它们对碳酸酐酶（CA）的抑制作用的 IC 值为 113 至 395.8 nM（K = 77.38-319.59 nM），对 hCA I 的抑制作用为 91.9 至 516 nM（K = 62.79-425.89 nM）。在这些化合物中，化合物 5c 对 hCA I 的活性最高（K ：77.38 nM），化合物 5g 对 hCA II 的活性最高（K ：62.79 nM）。
