Journal of enzyme inhibition and medicinal chemistry · 2020
Novel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties.
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Bilginer Sinan, Gonder Baris, Gul Halise Inci, Kaya Ruya, Gulcin Ilhami, Anil Baris, Supuran Claudiu T
Аннотация
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. KI 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 (KIs 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.