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- MakaleAçık Erişim2015N-Acylsulfonamides strongly inhibit human carbonic anhydrase isoenzymes i and II
Yildirim, Alper; Atmaca, Ufuk; Keskin, Ali; Topal, Meryem; Çelik, Murat; Gülçin, Ilhami; Supuran, Claudiu T.
Sulfonamides represent a significant class of biologically active compounds that inhibit carbonic anhydrase (CA, EC.: 4.2.1.1) isoenzymes involved in different pathological and physiological events. Sulfonamide CA inhibitors are used therapeutically as diuretic, antiglaucoma, antiobesity and anticancer agents. A series of new sulfonamides were synthesized using imides and tosyl chloride as starting materials. These N-acylsulfonamides efficiently inhibited the cytosolic human carbonic anhydrase isoenzymes I, and II (hCA I, and II), with nanomolar range inhibition constants ranging between 36.4 ± 6.0-254.6 ± 18.0 and 58.3 ± 0.6-273.3 ± 2.5 nM, respectively.