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- Title
Synthesis and Anticholinergic Activity of 4-hydroxycoumarin Derivatives Containing Substituted Benzyl-1,2,3-triazole Moiety.
- Authors
Bagheri, Sahar Mohammad; Khoobi, Mehdi; Nadri, Hamid; Moradi, Alireza; Emami, Saeed; Jalili ‐ Baleh, Leili; Jafarpour, Farnaz; Homayouni Moghadam, Farshad; Foroumadi, Alireza; Shafiee, Abbas
- Abstract
A series of 4-hydroxycoumarin-derived compounds 8a-p containing N-benzyl-1,2,3-triazole motif were designed as AChE inhibitors. The title compounds were obtained conveniently using multicomponent click reaction. The in vitro anticholinesterase evaluation of synthesized compounds against AChE and BuChE showed that some of them are potent and selective inhibitors of AChE. Among them, 2-chlorobenzyl derivative 8k showed the most potent activity against AChE ( IC50 = 0.18 μ m). Its activity was also superior to that of standard drug tacrine. The kinetic study and molecular docking simulation of the most potent compound 8k were also described.
- Subjects
PARASYMPATHOLYTIC agents; BIOSYNTHESIS; COUMARIN derivatives; TRIAZOLES; MOIETIES (Chemistry); ACETYLCHOLINESTERASE inhibitors; ALZHEIMER'S disease treatment
- Publication
Chemical Biology & Drug Design, 2015, Vol 86, Issue 5, p1215
- ISSN
1747-0277
- Publication type
Article
- DOI
10.1111/cbdd.12588