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目的为了研究硫色满-4-酮衍生物对乙酰胆碱酯酶的活性作用。方法采用取代的苯硫酚为原料,经取代反应和浓硫酸环合反应制备了6-羟基硫色满-4-酮,与苄基哌嗪反应制备3-(4-苄基哌嗪-1-甲基)硫色满-4-酮Mannich碱类盐酸盐,并将其用于乙酰胆碱酯酶(AChE)体外活性抑制实验。结果目标化合物具有AChE抑制活性,在微摩尔范围内,化合物8a的IC50=0.96μmol·L-1,优于对照组利斯的明。结论 3-(4-苄基哌嗪-1-甲基)硫色满-4-酮Mannich碱对乙酰胆碱酯酶有抑制活性,有进一步研究意义。
Aim To study the activity of thiochroman-4-one derivatives on acetylcholinesterase activity. Methods The substituted thiophenols were used as starting materials to prepare 6-hydroxythiochroman-4-one by the reaction of substitution and the reaction of concentrated sulfuric acid and the reaction with benzylpiperazine to prepare 3- (4-benzylpiperazine-1 -methyl) thiochroman-4-one Mannich base hydrochloride and used for in vitro activity inhibition experiments of acetylcholinesterase (AChE). Results The target compounds showed AChE inhibitory activity. IC50 of compound 8a was 0.96μmol·L-1 in the micromolar range, which was better than that of the control group. Conclusion The inhibitory activity of 3- (4-benzylpiperazin-1-yl) thiochroman-4-one Mannich base on acetylcholinesterase has further research significance.