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- Title
Design, Synthesis, Biological Evaluation, and Docking Study of Acetylcholinesterase Inhibitors: New Acridone-1,2,4-oxadiazole-1,2,3-triazole Hybrids.
- Authors
Mohammadi ‐ Khanaposhtani, Maryam; Mahdavi, Mohammad; Saeedi, Mina; Sabourian, Reyhaneh; Safavi, Maliheh; Khanavi, Mahnaz; Foroumadi, Alireza; Shafiee, Abbas; Akbarzadeh, Tahmineh
- Abstract
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 antiacetylcholinesterase 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.
- Subjects
MOLECULAR docking; ACETYLCHOLINESTERASE inhibitors; DRUG synthesis; DRUG design; OXADIAZOLES; TRIAZOLE derivatives
- Publication
Chemical Biology & Drug Design, 2015, Vol 86, Issue 6, p1425
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.12609