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Novel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties
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Novel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties
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Journal Article
Novel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties
2020
Overview
A series of compounds incorporating 3-(3-(2/3/4-substituted phenyl)triaz-1-en-1-yl) benzenesulfonamide moieties were synthesised and their chemical structure was confirmed by physico-chemical methods. Carbonic anhydrase (CA, EC 4.2.1.1) inhibitory effects of the compounds were evaluated against human isoforms hCA I and II. K
I
values of these sulphonamides were in the range of 21 ± 4-72 ± 2 nM towards hCA I and in the range of 16 ± 6-40 ± 2 nM against hCA II. The 4-fluoro substituted derivative might be considered as an interesting lead due to its effective inhibitory action against both hCA I and hCA II (K
I
s of 21 nM), a profile rarely seen among other sulphonamide CA inhibitors, making it of interest in systems where the activity of the two cytosolic isoforms is dysregulated.
Publisher
Taylor & Francis,Taylor & Francis Ltd,Taylor & Francis Group
Subject
/ Carbonic Anhydrase I - antagonists & inhibitors
/ Carbonic Anhydrase I - metabolism
/ Carbonic Anhydrase II - antagonists & inhibitors
/ Carbonic Anhydrase II - metabolism
/ Carbonic Anhydrase Inhibitors - chemical synthesis
/ Carbonic Anhydrase Inhibitors - chemistry
/ Carbonic Anhydrase Inhibitors - pharmacology
/ Dose-Response Relationship, Drug
/ Drugs
/ Enzymes
/ Glaucoma
/ Humans
/ Isoforms
/ NMR
/ Pharmacy
/ Structure-Activity Relationship
/ triazene
