6-氟硫色满酮Mannich碱的乙酰胆碱酯酶抑制活性及动力学研究

Study of 6-fluorothiochromanone Mannich bases inhibition activity and kinetics to acetylcholinesterase

目的研究6-氟硫色满酮Mannich碱对乙酰胆碱酯酶的抑制活性及作用类型。方法在体外采用Ellman方法对6-氟硫色满酮Mannich碱进行乙酰胆碱酯酶抑制实验和动力学实验。结果该化合物浓度为10-6mol/L时对乙酰胆碱酯酶的抑制率是51%,活性优于对照组利伐司替明,动力学实验初步证明是混合型竞争抑制。结论 6-氟硫色满酮Mannich碱作为乙酰胆碱酯酶抑制剂具有进一步研究价值。

Objective To study the inhibition activity and kinetics style of 6-fluorothiochromanone Mannich bases to acetylcholinesterase. Methods The inhibition and kinetics tests of 6-fluorothiochromanone Mannich bases to acetylcholinesterase were carried out by Ellman methods in vitro. Results The inhibition ratio of acetylcholinesterase was 51% when the concentration of this compound was 106mol/L, its inhibitive activity was better than Rivastigmine and primary kinetics experiments proved to be a mixed type of inhibition. Conclusion 6-fluorothiochromanones Mannich bases are worthy for further research in acetylcholinesterase inhibitors.