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  • Title: Synthesis of some new 3-coumaranone and coumarin derivatives as dual inhibitors of acetyl- and butyrylcholinesterase.
    Author: Alipour M, Khoobi M, Nadri H, Sakhteman A, Moradi A, Ghandi M, Foroumadi A, Shafiee A.
    Journal: Arch Pharm (Weinheim); 2013 Aug; 346(8):577-87. PubMed ID: 23852709.
    Abstract:
    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.
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