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- Title
Some N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido/thioureido]benzenesulfonamides as carbonic anhydrase I and II Inhibitors.
- Authors
TÜRK, Sevda; TOK, Fatih; ÇELİK, Hülya; KARAKUŞ, Sevgi; NADAROĞLU, Hayrunnisa; KOÇYİĞİT-KAYMAKÇIOĞLU, Bedia; KÜÇÜKOĞLU, Kaan
- 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, 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.
- Subjects
SUBSTITUENTS (Chemistry); BENZENESULFONAMIDES; CARBONIC anhydrase inhibitors; NUCLEAR magnetic resonance spectroscopy; ACETAZOLAMIDE
- Publication
Marmara Pharmaceutical Journal, 2017, Vol 21, Issue 1, p89
- ISSN
1309-0801
- Publication type
Article
- DOI
10.12991/marupj.259885