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Some N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido/ thioureido]benzenesulfonamides as carbonic anhydrase I and II Inhibitors

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10.12991-marupj.259885-226370.pdf (118.22 KB)

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2017

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In the present study, N-(5-methyl-1,3,4-thiadiazol-2-yl)- 4-[(3-substituted)ureido]benzenesulfonamide (1-9) and N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted) thioureido]benzenesulfonamide (10-14) derivatives were synthesized from 4-amino-N-(5-methyl-1,3,4-thiadiazol-2-yl) benzenesulfonamide (sulfamethizole). All new compounds were characterized by elemental analysis and various spectroscopic methods (FTIR, 1 H-NMR and MS). These new sulfonamide derivatives were investigated as inhibitors of carbonic anhydrase especially human carbonic anhydrase I and II. The new compounds showed higher activity against the human cytosolic CA I (IC50 values 0.144-15.65 nM) and CA II (IC50 values 0.109- 17.95 nM) in comparison with the clinically used CA inhibitor acetazolamide

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Carbonic anhydrase inhibitors, sulfonamide, sulfamethizole, urea and thiourea

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http://hdl.handle.net/11424/5279

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