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Heshmatollah Alinezhad

Heshmatollah Alinezhad

Academic rank: Professor
ORCID:
Education: PhD.
ScopusId:
Faculty: Faculty of Chemistry
Address:
Phone: 9111144735

Research

Title
Potent acetylcholinesterase inhibitors: Design, synthesis, biological evaluation, and docking study of acridone linked to 1,2,3-triazole derivatives
Type
JournalPaper
Keywords
Alzheimer's disease Acetylcholinesterase Acridone-1,2,3-triazole Docking study
Year
2015
Journal EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
DOI
Researchers Maryam Mohammadi-Khanaposhtani ، Mina Saeedi ، Narges Shamsaei Zafarghandi ، Mohammad Mahdavi ، Reyhaneh Sabourian ، Elahe K arimpour Razkenari ، Heshmatollah Alinezhad ، Mahnaz Khanavi ، Alireza Foroumadi ، Abbas Shafiee ، Tahmineh Akbarzadeh

Abstract

A novel series of acridone linked to 1,2,3-triazole derivatives have been synthesized and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities. The synthetic approach was started from the reaction of 2-bromobenzoic acid with aniline derivatives and subsequent cyclization reaction to give acridone derivatives. Then, reaction of the later compounds with propargyl bromide followed by azideealkyne cycloaddition reaction (click reaction) led to the formation of the title compounds in good yields. Among the synthesized compounds, 10-((1-(4-chlorobenzyl)-1H- 1,2,3-triazol-4-yl)methyl)-2-methoxyacridin-9(10H)-one 9g, depicted the most potent anti-AChE activity (IC50 ¼ 7.31 mM). Also, docking study confirmed the results obtained through in vitro experiments and predicted possible binding conformation.