Novel sulfamides as potential carbonic anhydrase isoenzymes inhibitors.

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Akincioglu A, Akbaba Y, Gocer H, Goksu S, Gulcin I, Supuran CT

Novel sulfamides as potential carbonic anhydrase isoenzymes inhibitors.

Bioorg Med Chem. 2013 Mar 15;21(6):1379-85. doi: 10.1016/j.bmc.2013.01.019. Epub 2013 Jan 22.

PubMed ID
23394864 [ View in PubMed
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Abstract

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 Ki of 0.45muM against hCA I and of 1.07muM against hCA II.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
AcetazolamideCarbonic anhydrase 1Ki (nM)36200N/AN/ADetails
AcetazolamideCarbonic anhydrase 2Ki (nM)3700N/AN/ADetails