Repository of Research and Investigative Information

Repository of Research and Investigative Information

Shahid Sadoughi University of Medical Sciences

Synthesis and Evaluation of Chroman-4-One Linked to <i>N</i>-Benzyl Pyridinium Derivatives as New Acetylcholinesterase Inhibitors

(2015) Synthesis and Evaluation of Chroman-4-One Linked to <i>N</i>-Benzyl Pyridinium Derivatives as New Acetylcholinesterase Inhibitors. Archiv der Pharmazie. pp. 643-649. ISSN 0365-6233

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Abstract

A novel series of chroman-4-one derivatives containing the N-benzyl pyridinium moiety were designed, synthesized, and evaluated for their acetylcholinesterase (AChE) inhibitory activities. Among the various synthesized compounds, (E)-1-(2,3-dibromobenzyl)-4-((7-ethoxy-4-oxochroman-3-ylidene)methyl)pyridinium bromide (8l) depicted the most potent anti-AChE activity (IC50=0.048M). In addition, the molecular modeling study allowed us to detect possible binding modes that are in full compliance with the observed results through in vitro experiments.

Item Type: Article
Keywords: Acetylcholinesterase Alzheimer's disease Chroman-4-one Docking study N-Benzyl pyridinium beta-amyloid aggregation alzheimers-disease anticholinesterase activity binding design cholinesterases docking potent Pharmacology & Pharmacy Chemistry
Page Range: pp. 643-649
Journal or Publication Title: Archiv der Pharmazie
Journal Index: WoS
Volume: 348
Number: 9
Identification Number: https://doi.org/10.1002/ardp.201500149
ISSN: 0365-6233
Depositing User: Mr mahdi sharifi
URI: http://eprints.ssu.ac.ir/id/eprint/29669

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