Design, synthesis and evaluation of new L-phenylalanine derivatives as acetylcholinesterase inhibitors / 中国药学杂志

ABSTRACT

OBJECTIVE: To research the effect of new L-phenylalanine derivatives on acetylcholinesterase (AChE) activity. METHODS: New L-phenylalanine derivatives were synthesized from substituted 2-bromo-l-acetophenones by four steps reaction, and their inhibitory activities on AChE were measured by Ellman method in vitro. RESULTS: The evaluation results showed that most derivatives possessed AChE inhibitory effect and the activity of compound 8b was the most potent with an IC50 value of 8.73 × 10-6 mol · L-1, which was more potent than that of rivastigmine; moreover, compound 8b had no inhibitory activities to BuChE. CONCLUSION: The inhibitory activities of new L-phenylalanine derivatives on acetylcholinesterase are worth studying further.