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新型4-[(3-环己基-4-芳基-2,3-二氢-1,3-噻唑-2-亚基)氨基]苯-1-磺酰胺的合成及其对碳酸酐酶I、II、IX、XII的抑制活性

New 4-[(3-cyclohexyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides, synthesis and inhibitory activity toward carbonic anhydrase I, II, IX, XII.

作者信息

Meleddu Rita, Maccioni Elias, Distinto Simona, Bianco Giulia, Melis Claudia, Alcaro Stefano, Cottiglia Filippo, Ceruso Mariangela, Supuran Claudiu T

机构信息

Department of Life and Environmental Sciences, University of Cagliari, Via Ospedale 72, 09124 Cagliari, Italy.

Department of Life and Environmental Sciences, University of Cagliari, Via Ospedale 72, 09124 Cagliari, Italy.

出版信息

Bioorg Med Chem Lett. 2015 Aug 15;25(16):3281-4. doi: 10.1016/j.bmcl.2015.05.076. Epub 2015 May 30.

Abstract

A series of 4-[(3-cyclohexyl-4-aryl-2,3-dihydro-1,3-thiazol-2-ylidene)amino]benzene-1-sulfonamides was synthesised and the activity of the new compounds as inhibitors of hCA I, II, IX, and XII was evaluated. These new derivatives exhibited some peculiarities with respect to previously reported sulfonamide based inhibitors of CA. We observed that the nature of the substituents in the position 3 and 4 of the dihydro-thiazole ring was relevant in determining both activity and selectivity profiles.

摘要

合成了一系列4-[(3-环己基-4-芳基-2,3-二氢-1,3-噻唑-2-亚基)氨基]苯-1-磺酰胺,并评估了这些新化合物作为hCA I、II、IX和XII抑制剂的活性。相对于先前报道的基于磺酰胺的CA抑制剂,这些新衍生物表现出一些独特之处。我们观察到,二氢噻唑环3位和4位取代基的性质对于确定活性和选择性概况都很重要。

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