Mohammadi-Khanaposhtani M, Mahdavi M, Saeedi M, Sabourian R, Safavi M, Khanavi M, Foroumadi A, Shafiee A, Akbarzadeh T.
Chem Biol Drug Des2015; 86: 1425–1432 (ISI, 2.48)

In this study, novel acridone-1,2,4-oxadiazole-1,2,3-triazole hybrids were designed, synthesized, and evaluated for their acetylcholinesterase and butyrylcholinesterase inhibitory activity. Among various synthesized compounds, 10-((1-((3-(4-methoxyphenyl)-1,2,4-oxadiazol-5-yl)methyl)-1H-1,2,3-triazol-4-yl)methyl)acridin-9(10H)-one 10b showed the most potent anti-acetylcholinesterase activity (IC50 = 11.55 μm) being as potent as rivastigmine. Also docking outcomes were in good agreement with in vitro results confirming the dual binding inhibitory activity of compound 10b.

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