Design, synthesis and evaluation of thiochroman-4-ones as acetylcholinesterase inhibitors / 中国药学杂志

ABSTRACT

OBJECTIVE: To research the effect of thiochroman-4-one derivatives on acetylcholine esterase activity. METHODS: Substituted thiophenols as the starting materials were transformed into 6-hydroxythiochroman-4-ones by substitution reaction and cycliza-tion reaction with concentrated sulfuric acid, and the resultant compounds were reacted with benzylpiperazins to prepare 3-(4-benzylpiperazine-1-methyl) thiochroman-4-ones hydrochloride, and their bioactivities as AChE inhibitors were measured in vitro. RESULTS: The target compounds had AChE inhibitive activity in micromolar range, and compound 8a was better than rivastigmine with IC50=0.96 μmol · L-1. CONCLUSION: 3-(4-Benzylpiperazine-1-methyl) thiochroman-4-ones show anti-acetylcholinesterase activity in vitro, which are worth further research.