Some N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido/thioureido]benzenesulfonamides as carbonic anhydrase I and II Inhibitors
MARMARA PHARMACEUTICAL JOURNAL, vol.21, no.1, pp.89-95, 2017 (ESCI, Scopus, TRDizin)
- Publication Type: Article / Article
- Volume: 21 Issue: 1
- Publication Date: 2017
- Doi Number: 10.12991/marupj.259885
- Journal Name: MARMARA PHARMACEUTICAL JOURNAL
- Journal Indexes: Emerging Sources Citation Index (ESCI), Scopus, TR DİZİN (ULAKBİM)
- Page Numbers: pp.89-95
- Open Archive Collection: AVESIS Open Access Collection
- Karadeniz Technical University Affiliated: No
Abstract
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, H-1-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.