Potent acetylcholinesterase inhibitors: design, synthesis, and structure–Activity relationships of bis-interacting ligands in the galanthamine series Original Research Article

New galanthamine derivatives, especially bis-interacting ligands 3–5 and 7–9 were prepared in order to interact with the catalytic and the peripheral sites of acetylcholinesterase (AChE). The synthesis, the anticholinesterase activities, and the structure–activity relationships of bis-interacting ligands are reported. Compounds 4d–e were found to be more potent than galanthamine and tacrine in inhibiting AChE.