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Synthesis of Some New 3‐ C oumaranone and Coumarin Derivatives as Dual Inhibitors of Acetyl‐ and Butyrylcholinesterase
Author(s) -
Alipour Masoumeh,
Khoobi Mehdi,
Nadri Hamid,
Sakhteman Amirhossein,
Moradi Alireza,
Ghandi Mehdi,
Foroumadi Alireza,
Shafiee Abbas
Publication year - 2013
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201300080
Subject(s) - butyrylcholinesterase , chemistry , acetylcholinesterase , coumarin , moiety , stereochemistry , aché , phenacyl , pyridinium , docking (animal) , enzyme , biochemistry , organic chemistry , medicine , nursing
A novel series of coumarin and 3‐coumaranone derivatives encompassing the phenacyl pyridinium moiety were synthesized and evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity using Ellman's method. All compounds presented inhibitory activity against both AChE and BuChE in the micromolar range. The molecular docking simulations revealed that all compounds were dual binding site inhibitors of AChE. A kinetic study was performed and the mechanism of enzyme inhibition was proved to be of mixed type. All compounds were tested for their antioxidant activity and no significant activity was observed.