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目的研究新型L-苯丙氨酸类化合物对乙酰胆碱酯酶活性的作用。方法以α-溴代苯乙酮为原料,经4步反应合成了新型L-苯丙氨酸类化合物,并采用Ellman分光光度法测定了它们对乙酰胆碱酯酶的体外抑制活性。结果所得大部分化合物均对乙酰胆碱酯酶有一定的乙酰胆碱酯酶体外抑制活性,其中化合物8b的活性最强,其IC50达到了8.73×10-6mol·L-1,优于对照药物利斯的明;但所得化合物对丁酰胆碱酯酶几乎没有抑制作用。结论所得L-苯丙氨酸类化合物对乙酰胆碱酯酶有一定的抑制活性,该类化合物对乙酰胆碱酯酶的抑制作用具有进一步研究的意义。
Objective To study the effect of novel L-phenylalanine on acetylcholinesterase activity. Methods Novel α-bromoacetophenones were synthesized by 4 steps using L-phenylalanine as starting materials and their inhibitory activities against acetylcholinesterase were determined by Ellman spectrophotometry. Results Most of the compounds showed acetylcholinesterase inhibitory activity against acetylcholinesterase in vitro. Among them, compound 8b had the strongest activity with IC50 of 8.73 × 10-6mol·L-1, which was better than that of the control drug Lees ; But the compound obtained almost no inhibition of butyrylcholinesterase. Conclusion The obtained L-phenylalanine compounds have certain inhibitory activity on acetylcholinesterase and the inhibitory effect of these compounds on acetylcholinesterase has further significance.