title: N-Acylsulfonamides strongly inhibit human carbonic anhydrase isoenzymes I and II.
abstract: 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.
authors: Faculty of Science, Department of Chemistry, Atatürk University, 25240 Erzurum, Turkey.
authors: Alper
authors: A
authors: Yıldırım
authors: Faculty of Science, Department of Chemistry, Atatürk University, 25240 Erzurum, Turkey.
authors: Ufuk
authors: U
authors: Atmaca
authors: Faculty of Science, Department of Chemistry, Atatürk University, 25240 Erzurum, Turkey.
authors: Ali
authors: A
authors: Keskin
authors: Gumushane University, Vocational School of Health Services, Department of Medical Services and Techniques, Gumushane, Turkey.
authors: Meryem
authors: M
authors: Topal
authors: Faculty of Science, Department of Chemistry, Atatürk University, 25240 Erzurum, Turkey. Electronic address: mcelik@atauni.edu.tr.
authors: Murat
authors: M
authors: Çelik
authors: Faculty of Science, Department of Chemistry, Atatürk University, 25240 Erzurum, Turkey; Department of Zoology, College of Science, King Saud University, Riyadh, Saudi Arabia.
authors: İlhami
authors: İ
authors: Gülçin
authors: Università degli Studi di Firenze, Neurofarba Department, Rm. 66, via U. Schiff 6, I-50019 Sesto Fiorentino (Firenze), Italy.
authors: Claudiu T
authors: CT
authors: Supuran
mesh_terms: D024401:Carbonic Anhydrase I / Q000037:antagonists & inhibitors*; D024402:Carbonic Anhydrase II / Q000037:antagonists & inhibitors*; D002257:Carbonic Anhydrase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry*; D006801:Humans; D007094:Imides / Q000737:chemistry; D007700:Kinetics; D015394:Molecular Structure; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry*; D014105:Tosyl Compounds / Q000737:chemistry
chemical_list: D002257:Carbonic Anhydrase Inhibitors; D007094:Imides; D013449:Sulfonamides; D014105:Tosyl Compounds; C025506:4-toluenesulfonyl chloride; D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II
keywords: Carbonic anhydrase; Enzyme inhibition; Enzyme purification; Imide; N-Acylsulfonamide; Sulfonamide