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 IC₅₀ (hydratese) and inhibition constant values (K_i, esterase) were determined. All studied compounds exhibited potent inhibition against these enzymes. They inhibited carbonic anhydrases (CAs) with the IC₅₀ values of 113 to 395.8 nM (K_i = 77.38‐319.59 nM) for hCA I and 91.9 to 516 nM (K_i = 62.79‐425.89 nM) for hCA II. Among the compounds, 5c was found to be the most active one (K_i: 77.38 nM) for hCA I and 5g was found for hCA II with the value of 62.79 nM.

中文翻译：

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作为碳酸酐酶抑制剂的新系列噻唑-（2（3H）-亚烷基氨基）苯磺酰胺衍生物的合成。

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（3 H）-亚烷基氨基）苯磺酰胺衍生物，还确定了一些抑制参数，包括IC ₅₀（水合）和抑制常数（K _i，酯酶）。所有研究的化合物均显示出对这些酶的有效抑制作用。他们抑制了碳酸酐酶（CAs）， hCA I的IC ₅₀值为113至395.8 nM（K _i = 77.38-319.59 nM）， 而hCA II的IC ₅₀值为91.9至516 nM（K _i = 62.79-425.89 nM）。在化合物中，5c被认为是最活跃的一个（ķ_我：77.38 nM）的为HCA I和5克被发现的HCA与II 62.79 NM的值。