Synthesis and anticholinergic activity of 4‐hydroxycoumarin derivatives containing substituted benzyl‐1, 2, 3‐triazole moiety
Chemical biology & drug design, 2015•Wiley Online Library
A series of 4‐hydroxycoumarin‐derived compounds 8a‐p containing N‐benzyl‐1, 2, 3‐
triazole motif were designed as AC hE inhibitors. The title compounds were obtained
conveniently using multicomponent click reaction. The in vitro anticholinesterase evaluation
of synthesized compounds against AC hE and BuChE showed that some of them are potent
and selective inhibitors of AC hE. Among them, 2‐chlorobenzyl derivative 8k showed the
most potent activity against AC hE (IC 50= 0.18 μm). Its activity was also superior to that of …
triazole motif were designed as AC hE inhibitors. The title compounds were obtained
conveniently using multicomponent click reaction. The in vitro anticholinesterase evaluation
of synthesized compounds against AC hE and BuChE showed that some of them are potent
and selective inhibitors of AC hE. Among them, 2‐chlorobenzyl derivative 8k showed the
most potent activity against AC hE (IC 50= 0.18 μm). Its activity was also superior to that of …
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.
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