Novel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties
Özet
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.
Anahtar kelimeler
Atıf için künye
Bilginer, S., Gonder, B., Gül, H. İ., Kaya, R., Gülçin, İ., Anıl, B., & Supuran, C. T. (2020). Novel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 35(1), 325–329. https://doi.org/10.1080/14756366.2019.1700240
BibTeX
@article{bilginer2020-19882,
author = {Bilginer, Sinan and Gonder, Baris and Gül, Halise İnci and Kaya, Ruya and Gülçin, İlhami and Anıl, Barış and Supuran, Claudiu T.},
title = {Novel sulphonamides incorporating triazene moieties show powerful carbonic anhydrase I and II inhibitory properties},
journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
year = {2020},
volume = {35},
number = {1},
pages = {325--329},
issn = {1475-6366},
doi = {10.1080/14756366.2019.1700240},
url = {https://akademik.atauni.edu.tr/yayinlar/19882-novel-sulphonamides-incorporating-triazene-moieties-show-powerful-carbonic}
}