Ureidobenzenesulfonamides as Selective Carbonic Anhydrase I, IX, and XII Inhibitors

Sulfonamides remain an important class of drugs, especially because of their inhibitory effects on carbonic anhydrases. Herein, we have synthesized several sulfonamides and tested them for their inhibitory activity against carbonic anhydrases hCA I, hCA II, hCA IX, and hCA XII, respectively. Thereby...

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Bibliographic Details
Main Authors: Toni C. Denner, Andrea Angeli, Marta Ferraroni, Claudiu T. Supuran, René Csuk
Format: Article
Language:English
Published: MDPI AG 2023-11-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/28/23/7782
Description
Summary:Sulfonamides remain an important class of drugs, especially because of their inhibitory effects on carbonic anhydrases. Herein, we have synthesized several sulfonamides and tested them for their inhibitory activity against carbonic anhydrases hCA I, hCA II, hCA IX, and hCA XII, respectively. Thereby, biphenyl- and benzylphenyl-substituted sulfonamides showed high selectivity against hCA IX and hCA XII; these enzymes are common targets in the treatment of hypoxic cancers, and noteworthy inhibitory activity was observed for several compounds toward hCA I that might be of interest for future applications to treat cerebral edema. Compound <b>3</b> (4-[3-(2-benzylphenyl)ureido]benzenesulfonamide) held an exceptionally low K<sub>i</sub> value of 1.0 nM for hCA XII.
ISSN:1420-3049