Editor-in-Chief
Hatice Kübra Elçioğlu
Vice Editors
Levent Kabasakal
Esra Tatar
Online ISSN
2630-6344
Publisher
Marmara University
Frequency
Bimonthly (Six issues / year)
Abbreviation
J.Res.Pharm.
Former Name
Marmara Pharmaceutical Journal
Marmara Pharmaceutical Journal
2017 , Vol 21 , Issue 1
Some N-(5-Methyl-1,3,4-Thiadiazol-2-yl)-4-[(3-Substituted)Ureido/ Thioureido]Benzenesulfonamides as Carbonic Anhydrase I and II Inhibitors
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, 34668, Istanbul, TURKEY2Department of Pharmaceutical Technology, Faculty of Pharmacy, Agri Ibrahim Cecen University, 04000, Agri, TURKEY
3Department of Food Technology, Erzurum Vocational School, Ataturk University, 25240, Erzurum, TURKEY
4Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ataturk University, 25240, Erzurum, TURKEY DOI : 10.12991/marupj.259885 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, 1H-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. Keywords : Carbonic anhydrase inhibitors, sulfonamide, sulfamethizole, urea and thiourea