Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids

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‐triazo...

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Veröffentlicht in:Chemical biology & drug design 2015-12, Vol.86 (6), p.1425-1432
Hauptverfasser: Mohammadi-Khanaposhtani, Maryam, Mahdavi, Mohammad, Saeedi, Mina, Sabourian, Reyhaneh, Safavi, Maliheh, Khanavi, Mahnaz, Foroumadi, Alireza, Shafiee, Abbas, Akbarzadeh, Tahmineh
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Sprache:eng
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Zusammenfassung: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. A novel series of acridone‐1,2,4‐oxadiazole‐1,2,3‐triazole hybrids were synthesized and evaluated in vitro for their acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities.
ISSN:1747-0277
1747-0285
DOI:10.1111/cbdd.12609