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

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. 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.

authors

Bilginer S,Gonder B,Gul HI,Kaya R,Gulcin I,Anil B,Supuran CT

doi

10.1080/14756366.2019.1700240

subject

Has Abstract

pub_date

2020-12-01 00:00:00

pages

325-329

issue

1

eissn

1475-6366

issn

1475-6374

journal_volume

35

pub_type

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