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A class of sulfonamides as carbonic anhydrase I and II inhibitors

机译:一类磺酰胺作为碳酸酐酶I和II抑制剂

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Four groups of novel sulfonamide derivatives: (i) acetoxybenzamide, (ii) triacetoxybenzamide, (iii) hydroxybenzamide and (iv) trihydroxybenzamide, all having thiazole, pyrimidine, pyridine, isoxazole and thiadiazole moieties were prepared and their inhibitory effects were studied on two metalloenzymes, i.e. carbonic anhydrase isozymes (hCA I and II), purified from human erythrocyte cells by Sepharose-4B-l-tyrosine-sulfanilamide affinity chromatography. These enzymes are present in almost all living organisms to catalyse the synthesis of bicarbonate ion (HCO3-) from carbon dioxide and water. The sulfonamide derivatives were found to be active against hCA I and II in the range of 2.62-136.54 and 5.74-210.58nM, respectively.
机译:四组新的磺酰胺衍生物:(i)乙酰氧基苯甲酰胺,(ii)制备羟基苯甲酰胺,(III)羟基苯甲酰胺和(IV)三唑氧酰胺,所有具有噻唑,嘧啶,吡啶,异恶唑和噻唑部分,并在两种金属酶上研究了它们的抑制作用 ,通过Sepharose-4b-L-酪氨酸 - 磺胺亲和力层析从人红细胞细胞纯化,即碳酸酐酶同工酶(HCA I和II)。 这些酶存在于几乎所有生物体中,以催化来自二氧化碳和水的碳酸氢盐离子(HCO3-)的合成。 发现磺酰胺胺衍生物分别在2.62-136.54和5.74-210.58nm的范围内对HC 8和II有效。

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