Synthesis, carbonic anhydrase I and II inhibition studies of the 1,3,5-trisubstituted-pyrazolines
Özet
4-(3-(4-Substituted-phenyl)-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl) benzenesulfonamides (9-16) were successfully synthesized and their chemical structures were confirmed by H-1 NMR, C-13 NMR, and HRMS spectra. Carbonic anhydrase I and II inhibitory effects of the compounds were investigated. Ki values of the compounds were in the range of 316.7 +/- 9.6-533.1 +/- 187.8nM towards hCA I and 412.5 +/- 115.4-624.6 +/- 168.2nM towards hCA II isoenzymes. While K-i values of the reference compound Acetazolamide were 278.8 +/- 44.3 nM and 293.4 +/- 46.4 nM towards hCA I and hCA II izoenzymes, respectively. Compound 14 with bromine and compound 13 with fluorine substituents can be considered as the leader compounds of the series because of the lowest K-i values in series to make further detailed carbonic anhydrase inhibiton studies.
Anahtar kelimeler
Atıf için künye
Gül, H. İ., Mete, E., TASLIMI, P., Gülçin, İ., & SUPURAN, C. T. (2017). Synthesis, carbonic anhydrase I and II inhibition studies of the 1,3,5-trisubstituted-pyrazolines. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 32(1), 189–192. https://doi.org/10.1080/14756366.2016.1244533
BibTeX
@article{gul2017-19927,
author = {Gül, Halise İnci and Mete, Ebru and TASLIMI, Parham and Gülçin, İlhami and SUPURAN, Claudiu T.},
title = {Synthesis, carbonic anhydrase I and II inhibition studies of the 1,3,5-trisubstituted-pyrazolines},
journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
year = {2017},
volume = {32},
number = {1},
pages = {189--192},
issn = {1475-6366},
doi = {10.1080/14756366.2016.1244533},
url = {https://akademik.atauni.edu.tr/yayinlar/19927-synthesis-carbonic-anhydrase-i-and-ii-inhibition-studies-of-the-135}
}