Ureidobenzenesulfonamides as efficient inhibitors of carbonic anhydrase II

[Display omitted] •Glaucoma is among the leading causes for irreversible blindness.•It is expected that by 2040 111.8 million persons will suffer from this disease.•Carbanhydrase II inhibitors are in use as anti-glaucoma agents.•Several novel ureidobenzenesulfonamides are efficient inhibitors of thi...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic chemistry 2019-10, Vol.91, p.103123-103123, Article 103123
Main Authors: Serbian, Immo, Schwarzenberger, Philipp, Loesche, Anne, Hoenke, Sophie, Al-Harrasi, Ahmed, Csuk, René
Format: Article
Language:English
Subjects:
Carbonic anhydrase
Glaucoma
Inhibitor
Urea
Ureidobenzenesulfonamide
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:[Display omitted] •Glaucoma is among the leading causes for irreversible blindness.•It is expected that by 2040 111.8 million persons will suffer from this disease.•Carbanhydrase II inhibitors are in use as anti-glaucoma agents.•Several novel ureidobenzenesulfonamides are efficient inhibitors of this enzyme.•A benzylphenyl substituted sulfonamide cytotoxic to colorectal carcinoma cells HT29. Sulfonamides represent an important class of drugs because of their inhibitory effect on carbonic anhydrases (CAs). We therefore synthesized several ureidobenzenesulfonamides and evaluated their bCA II inhibition for their potential use as anti-glaucoma gents. Since these compounds must not show cytotoxic effects, their cytotoxic potential against several human tumor cell lines and non-malignant fibroblasts was investigated. Several fluorophenyl substituted sulfonamides were efficient inhibitors of bCA II. Only one benzylphenyl substituted sulfonamide, however, showed a remarkable selectivity for HT29 colorectal carcinoma cells while being significantly less cytotoxic to non-malignant fibroblasts.
ISSN:0045-2068
1090-2120
DOI:10.1016/j.bioorg.2019.103123