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Title
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Synthesis and structure-activity relationship study of benzofuranbased chalconoids bearing benzylpyridinium moiety as potent acetylcholinesterase inhibitors
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Type
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JournalPaper
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Keywords
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Acetylcholinesterase Alzheimer's disease Benzofuran Docking study Pyridinium
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Abstract
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A series of benzofuran-based chalconoids 6aev were designed and synthesized as new potential AChE inhibitors. The in vitro assay of synthesized compounds 6aev showed that most compounds had significant anti-AChE activity at micromolar or sub-micromolar levels. Among the tested compounds, 3- pyridinium derivative 6m bearing N-(2-bromobenzyl) moiety and 7-methoxy substituent on the benzofuran ring exhibited superior activity. This compound with IC50 value of 0.027 mM was as potent as standard drug donepezil.
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Researchers
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Abbas Shafiee (Not In First Six Researchers), Alireza Foroumadi (Not In First Six Researchers), Heshmatollah Alinezhad (Not In First Six Researchers), Saeed Emami (Not In First Six Researchers), Hamid Nadri (Fifth Researcher), Alireza Moradi (Fourth Researcher), Mohammad Mahdavi (Third Researcher), Ghodsi Mohammadi Ziarani (Second Researcher), Manizheh Mostofi (First Researcher)
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