Synthesis and carbonic anhydrase inhibitory activities of new thienyl-substituted pyrazoline benzenesulfonamides
Özet
A series of new thienyl-substituted pyrazoline benzenesulfonamides were synthesized and their carbonic anhydrase (CA, EC 4.2.1.1) inhibitory activities were tested on the human (h) isoforms hCA I and hCA II. The inhibition constant (K-i) of these sulfonamides were in the range of 232.16-637.70nM toward the slow cytosolic isozyme hCA I, and in the range of 342.07-455.80nM toward hCA II. Many of these compounds showed comparable inhibition with the reference sulfonamide acetazolamide, a clinically used drug. As the sulfonamide CA inhibitors (CAIs) show many therapeutic uses, these derivatives represent interesting examples of a novel class of such derivatives.
Anahtar kelimeler
Atıf için künye
Mete, E., COMEZ, B., Gül, H. İ., Gülçin, İ., & SUPURAN, C. T. (2016). Synthesis and carbonic anhydrase inhibitory activities of new thienyl-substituted pyrazoline benzenesulfonamides. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 31, 1–5. https://doi.org/10.1080/14756366.2016.1181627
BibTeX
@article{mete2016-19911,
author = {Mete, Ebru and COMEZ, Birnur and Gül, Halise İnci and Gülçin, İlhami and SUPURAN, Claudiu T.},
title = {Synthesis and carbonic anhydrase inhibitory activities of new thienyl-substituted pyrazoline benzenesulfonamides},
journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
year = {2016},
volume = {31},
pages = {1--5},
issn = {1475-6366},
doi = {10.1080/14756366.2016.1181627},
url = {https://akademik.atauni.edu.tr/yayinlar/19911-synthesis-and-carbonic-anhydrase-inhibitory-activities-of-new-thienyl}
}