Publication:
Some N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-substituted)ureido/thioureido]benzenesulfonamides as carbonic anhydrase I and II Inhibitors

Thumbnail Image

Files

Türk et al. - 2016 - Some N-(5-methyl-1,3,4-thiadiazol-2-yl)-4-[(3-subs.pdf (118.22 KB)

Date

2016-08-25

Authors

Journal Title

Journal ISSN

Volume Title

Publisher

MARMARA UNIV, FAC PHARMACY

Research Projects

Organizational Units

Journal Issue

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.

Description

Keywords

Carbonic anhydrase inhibitors, sulfonamide, sulfamethizole, urea and thiourea, PURIFICATION, XII

Citation

URI

https://hdl.handle.net/11424/241811

Collections

Research Outputs