Some N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido/thioureido]benzenesulfonamides as carbonic anhydrase I and II Inhibitors
Özet
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.
Atıf için künye
TURK, S., TOK, F., ÇELİK, H., KARAKUŞ, S., Nadaroğlu, H., KAYMAKÇIOĞLU, B., & KÜÇÜKOĞLU, K. (2017). 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, 21(1), 89–95. https://doi.org/10.12991/marupj.259885
BibTeX
@article{turk2017-330234,
author = {TURK, S and TOK, FATİH and ÇELİK, HÜLYA and KARAKUŞ, SEVGİ and Nadaroğlu, Hayrunnisa and KAYMAKÇIOĞLU, BEDİA and KÜÇÜKOĞLU, KAAN},
title = {Some N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido/thioureido]benzenesulfonamides as carbonic anhydrase I and II Inhibitors},
journal = {MARMARA PHARMACEUTICAL JOURNAL},
year = {2017},
volume = {21},
number = {1},
pages = {89--95},
issn = {1309-0801},
doi = {10.12991/marupj.259885},
url = {https://akademik.atauni.edu.tr/yayinlar/330234-some-n-5-methyl-134-thiadiazol-2-yl-4-3}
}