Editor-in-Chief İlkay Küçükgüzel Associate Editor Aslı Türe 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
Sevda Türk1, Fatih Tok1, Hülya Çelik2,Sevgi Karakuş1, Hayrunnisa Nadaroğlu3, Bedia Koçyiğit-Kaymakçıoğlu1, Kaan Küçükoğlu4
1Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, 34668, Istanbul, TURKEY
2Department 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
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