Novel sulfamides as potential carbonic anhydrase isoenzymes inhibitors

作者：Akincioglu Akin; Akbaba Yusuf; Gocer Hulya; Goksu Suleyman^*; Gulcin Ilhami; Supuran Claudiu T

来源：Bioorganic & Medicinal Chemistry, 2013, 21(6): 1379-1385.

DOI：10.1016/j.bmc.2013.01.019

• Aminoindane
• Aminotetralin
• Sulfamide
• Carbonic anhydrase
• Inhibitors

Sulfamides represent an important class of biologically active compounds. A series of novel sulfamides were synthesized from 1-aminoindanes, 1-aminotetralin, 2-aminoindanes and 2-aminotetralin via the reactions of free amines, benzyl alcohol and chlorosulfonyl isocyanate (CSI) followed by hydrogenolysis of the obtained sulfamoylcarbamates. Carbonic anhydrase (CA, EC 4.2.1.1) inhibitory effects of the new sulfamides have been investigated. The human (h) isozymes hCA I and hCA II have been investigated in this study by using an esterase assay with 4-nitrophenyl acetate as substrate. The new sulfamides showed inhibition constants in the micro-submicromolar range, with one compound (N-(indane-1-yl) sulfamide) showing a K-i of 0.45 mu M against hCA I and of 1.07 mu M against hCA II.

• 出版日期2013-3-15