Title : Design and synthesis of novel coumarin-pyridinium hybrids: In vitro cholinesterase inhibitory activity - Vafadarnejad_2018_Bioorg.Chem_77_311 |
Author(s) : Vafadarnejad F , Mahdavi M , Karimpour-Razkenari E , Edraki N , Sameem B , Khanavi M , Saeedi M , Akbarzadeh T |
Ref : Bioorg Chem , 77 :311 , 2018 |
Abstract :
A novel series of coumarin-pyridinium hybrids were synthesized and evaluated as inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) using Ellman's method. Among synthesized compounds, 1-(3-fluorobenzyl)-4-((2-oxo-2H-chromene-3-carboxamido)methyl)pyridinium bromide (7l) was found to be the most active compound toward AChE (IC50=10.14microM), 1-(3-chlorobenzyl)-3-((2-oxo-2H-chromene-3-carboxamido)methyl)pyridinium bromide (7g) and 1-(2,3-dichlorobenzyl)-3-((2-oxo-2H-chromene-3-carboxamido)methyl)pyridinium chloride (7h) depicted the best BChE inhibitory activity (IC50s=0.32 and 0.43microM, respectively). Although most compounds showed moderate to good anti-AChE activity, their anti-BChE activity was more significant and compound 7g was found as the most selective BChE with SI of 101.18. Also, kinetic study of the compounds 7g and 7l displayed a mixed type inhibition for both AChE and BChE. Furthermore, they were evaluated against beta-secretase; however, they showed low inhibitory activity. |
PubMedSearch : Vafadarnejad_2018_Bioorg.Chem_77_311 |
PubMedID: 29421707 |
Vafadarnejad F, Mahdavi M, Karimpour-Razkenari E, Edraki N, Sameem B, Khanavi M, Saeedi M, Akbarzadeh T (2018)
Design and synthesis of novel coumarin-pyridinium hybrids: In vitro cholinesterase inhibitory activity
Bioorg Chem
77 :311
Vafadarnejad F, Mahdavi M, Karimpour-Razkenari E, Edraki N, Sameem B, Khanavi M, Saeedi M, Akbarzadeh T (2018)
Bioorg Chem
77 :311