Synthesis and anticholinergic activity of 4-hydroxycoumarin derivatives containing substituted benzyl-1,2,3-triazole moiety.

Synthesis and anticholinergic activity of 4-hydroxycoumarin derivatives containing substituted benzyl-1,2,3-triazole moiety.

Chemical biology & drug design (2015-05-27)

Sahar Mohammad Bagheri, Mehdi Khoobi, Hamid Nadri, Alireza Moradi, Saeed Emami, Leili Jalili-Baleh, Farnaz Jafarpour, Farshad Homayouni Moghadam, Alireza Foroumadi, Abbas Shafiee

PMID26010139

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 μm). 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.

MATERIALS

Product Number

Brand

Product Description

127698

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