Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors

A new series of galanthamine derivatives have been designed, synthesized and evaluated as acetylcholinesterase inhibitors. All of the new compounds prepared showed high AChE inhibitory activities, with compound 3e that has an N-hexyl-benzyl piperidine substituent on the nitrogen atom reaching the best inhibitory activity for AChE (IC50 = 5.62 nM). The docking study performed with AutoDock demonstrated that 3e was nicely accommodated by AChE.

Graphical abstractA new series of galanthamine derivatives were designed, synthesized and evaluated as acetylcholinesterase inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide