Novel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties.

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2020
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Abstract
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 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 (Ks 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.
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Authors Bilginer, Sinan;Gonder, Baris;Gul, Halise Inci;Kaya, Ruya;Gulcin, Ilhami;Anil, Baris;Supuran, Claudiu T;
Journal Journal of enzyme inhibition and medicinal chemistry
Year 2020
DOI
10.1080/14756366.2019.1700240
URL
Keywords
Inhibitors carbonic anhydrase diazonium salt metanilamide sulphonamide triazene

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