Synthesis of Some New 3‐Coumaranone and Coumarin Derivatives as Dual Inhibitors of Acetyl‐ and Butyrylcholinesterase. Issue 8 (15th July 2013)

• Record Type: Journal Article
• Authors: Alipour, Masoumeh; Khoobi, Mehdi; Nadri, Hamid; Sakhteman, Amirhossein; Moradi, Alireza; Ghandi, Mehdi; Foroumadi, Alireza; Shafiee, Abbas
• Is Part Of: Archiv der Pharmazie. Volume 346:Issue 8(2013:Aug.)
• Page Start: 577
• Page End: 587
• Publication Date: 2013-07-15
• Subjects: Pharmaceutical chemistry -- Periodicals; Pharmacology -- Periodicals; 615.19
• DOI: 10.1002/ardp.201300080
• Languages: English
• ISSNs: 0365-6233

Abstract

<abstract abstract-type="main" xml:lang="en"> <title> <x xml:space="preserve">Abstract</x> </title> <sec id="ardp201300080-sec-0001" sec-type="section"> <p>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.</p> </sec> </abstract>