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Title
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Potent acetylcholinesterase inhibitors: Design, synthesis, biological evaluation, and docking study of acridone linked to 1,2,3-triazole derivatives
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Type
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JournalPaper
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Keywords
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Alzheimer's disease Acetylcholinesterase Acridone-1,2,3-triazole Docking study
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Abstract
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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.
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Researchers
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Tahmineh Akbarzadeh (Not In First Six Researchers), Abbas Shafiee (Not In First Six Researchers), Alireza Foroumadi (Not In First Six Researchers), Mahnaz Khanavi (Not In First Six Researchers), Heshmatollah Alinezhad (Not In First Six Researchers), Elahe K arimpour Razkenari (Not In First Six Researchers), Reyhaneh Sabourian (Fifth Researcher), Mohammad Mahdavi (Fourth Researcher), Narges Shamsaei Zafarghandi (Third Researcher), Mina Saeedi (Second Researcher), Maryam Mohammadi-Khanaposhtani (First Researcher)
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