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Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone‐1,2,4‐oxadiazole‐1,2,3‐triazole Hybrids
Author(s) -
MohammadiKhanaposhtani Maryam,
Mahdavi Mohammad,
Saeedi Mina,
Sabourian Reyhaneh,
Safavi Maliheh,
Khanavi Mahnaz,
Foroumadi Alireza,
Shafiee Abbas,
Akbarzadeh Tahmineh
Publication year - 2015
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12609
Subject(s) - acridone , butyrylcholinesterase , acetylcholinesterase , oxadiazole , docking (animal) , chemistry , rivastigmine , triazole , stereochemistry , 1,2,3 triazole , cholinesterase , aché , combinatorial chemistry , enzyme , biochemistry , pharmacology , organic chemistry , biology , donepezil , medicine , dementia , nursing , disease , pathology
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)‐1 H ‐1,2,3‐triazol‐4‐yl)methyl)acridin‐9(10 H )‐one 10b showed the most potent anti‐acetylcholinesterase activity (IC 50 = 11.55 μ m ) 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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