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N-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.
Affiliation
  • Yildirim A; Faculty of Science, Department of Chemistry, Atatürk University, 25240 Erzurum, Turkey.
  • Atmaca U; Faculty of Science, Department of Chemistry, Atatürk University, 25240 Erzurum, Turkey.
  • Keskin A; Faculty of Science, Department of Chemistry, Atatürk University, 25240 Erzurum, Turkey.
  • Topal M; Gumushane University, Vocational School of Health Services, Department of Medical Services and Techniques, Gumushane, Turkey.
  • Çelik M; Faculty of Science, Department of Chemistry, Atatürk University, 25240 Erzurum, Turkey. Electronic address: mcelik@atauni.edu.tr.
  • Gülçin I; Faculty of Science, Department of Chemistry, Atatürk University, 25240 Erzurum, Turkey; Department of Zoology, College of Science, King Saud University, Riyadh, Saudi Arabia.
  • Supuran CT; Università degli Studi di Firenze, Neurofarba Department, Rm. 66, via U. Schiff 6, I-50019 Sesto Fiorentino (Firenze), Italy.
Bioorg Med Chem ; 23(10): 2598-605, 2015 May 15.
Article in En | MEDLINE | ID: mdl-25863492
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.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Sulfonamides / Carbonic Anhydrase Inhibitors / Carbonic Anhydrase I / Carbonic Anhydrase II Limits: Humans Language: En Journal: Bioorg Med Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2015 Document type: Article Affiliation country: Country of publication:
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Sulfonamides / Carbonic Anhydrase Inhibitors / Carbonic Anhydrase I / Carbonic Anhydrase II Limits: Humans Language: En Journal: Bioorg Med Chem Journal subject: BIOQUIMICA / QUIMICA Year: 2015 Document type: Article Affiliation country: Country of publication: