The inhibitory effects of phenolic Mannich bases on carbonic anhydrase I and II isoenzymes
Özet
Phenolic mono Mannich bases [2-[4-hydroxy-3-(aminomethyl) benzylidene]-2,3-dihydro-1H-inden-1-one (8-15)] and bis Mannich bases [2-[4-hydroxy-3,5-bis(aminomethyl) benzylidene]-2, 3-dihydro-1H-inden-1-one (2-7)] were synthesized starting from 2-(4-hydroxybenzylidene)-2, 3-dihydro-inden-1-one (1). This study was designed in order to investigate the carbonic anhydrase (CA, EC 4.2.1.1) inhibitory properties of a library of compounds incorporating the phenol functional group. All prepared compounds showed a low inhibition percentages on both human (h) isoforms hCA I and hCA II compared to the reference sulfonamide acetazolamide. Mannich bases 2-15 had lower inhibition percentages than the compound 1 on hCA I and hCA II, except compound 14, which is a Mannich base derivative of dipropylamine, which had a similar inhibitory power as compound 1 on hCA II. All compounds synthesized 1-15 were 1.3-1.9 times more effective on hCA II comparing with the effectivenes of the compounds on hCA I.
Anahtar kelimeler
Atıf için künye
YAMALI, C., TUĞRAK, M., Gül, H. İ., TANC, M., & SUPURAN, C. T. (2016). The inhibitory effects of phenolic Mannich bases on carbonic anhydrase I and II isoenzymes. JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, 31(6), 1678–1681. https://doi.org/10.3109/14756366.2015.1126715
BibTeX
@article{yamali2016-19877,
author = {YAMALI, Cem and TUĞRAK, Mehtap and Gül, Halise İnci and TANC, Muhammet and SUPURAN, Claudiu T.},
title = {The inhibitory effects of phenolic Mannich bases on carbonic anhydrase I and II isoenzymes},
journal = {JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY},
year = {2016},
volume = {31},
number = {6},
pages = {1678--1681},
issn = {1475-6366},
doi = {10.3109/14756366.2015.1126715},
url = {https://akademik.atauni.edu.tr/yayinlar/19877-the-inhibitory-effects-of-phenolic-mannich-bases-on-carbonic-anhydrase-i-and-ii}
}