Ataturk University, Science Faculty, Department of Chemistry, Erzurum, Turkey.
J Enzyme Inhib Med Chem. 2012 Dec;27(6):818-24. doi: 10.3109/14756366.2011.617745. Epub 2011 Dec 22.
The inhibition of two human cytosolic carbonic anhydrase (hCA, EC 4.2.1.1) isozymes I, II and human serum isozyme VI, with a series of tosylited aromatic amine derivatives was investigated. The K(I) ranges of compounds 1-14 and acetazolamide against hCA I ranged between 1.130 and- 448.2 μM, against hCA II between 0.103 and- 14.3 μM, and against hCA VI ranged between 0.340 and- 42.39 μM. Tosylited aromatic amine derivatives are thus interesting hCA I, II and VI inhibitors, and might be used as leads for generating enzyme inhibitors eventually targeting other isoforms which have not been assayed yet for their interactions with such agents.
研究了一系列对甲苯磺酰化芳胺衍生物对两种人胞质碳酸酐rase（hCA，EC 4.2.1.1）同工酶 I、II 和人血清同工酶 VI 的抑制作用。化合物 1-14 和乙酰唑胺对 hCA I 的 K(I)范围在 1.130 到-448.2 μM 之间，对 hCA II 的 K(I)范围在 0.103 到-14.3 μM 之间，对 hCA VI 的 K(I)范围在 0.340 到-42.39 μM 之间。因此，对甲苯磺酰化芳胺衍生物是有趣的 hCA I、II 和 VI 抑制剂，并且可能被用作产生酶抑制剂的先导物，最终针对尚未针对其与这些药物的相互作用进行测定的其他同工酶。
