Tryptamine–Triazole Hybrid Compounds for Selective Butyrylcholinesterase Inhibition

Tryptamine–triazole hybrid compounds ( 11 – 18 ) were synthesized via click reaction between tryptamine azide and propargylated natural compounds. Their cholinesterase inhibitory activity was evaluated. Among the eight compounds, compound 11 showed the most potent inhibitory activity [IC 50 = 0.42 ± 0.29 μM for equine butyrylcholinesterase (BuChE) and 1.96 ± 0.15 μM for human BuChE]. From the molecular modeling study, compound 11 was bound to...