丙炔苯丙胺类结构衍生物的合成与初步活性分析

Synthesis and preliminary analysis of the activity of N-benzyl-N-metylprop-2-yn-1-amine derivatives

目的设计合成丙炔苯丙胺类化合物。方法以3-甲基苯甲酸为原料,经过NBS溴代、氨解与缩合三步反应得到目标终产物。采用时间分辨荧光法对合成的3个目标化合物进行体外分子水平的活性评价。结果得到3个丙炔苯丙胺类衍生物,结构均经过1H NMR和LC-MS表征。结论合成的化合物未见文献报道,探索的合成路线稳定可靠,操作简单。3个化合物对β-分泌酶没有明显的抑制活性。

Objective To design and synthesize N-benzyl-N-metylprop-2-yn-1amine derivatives. Methods 3-methyl-benzoic acid was used as a raw material and we finish the synthesis through bromination,ammonolysis and condensation reaction. Time-resolved fluorescence was used to evaluate the inhibitory activity of these compounds againstβ-secretase. Results Three compounds were synthe-sized and the structures were confirmed by 1H NMR and LC-MS characterization. Conclusion The synthesized compounds have not been reported before and the synthetic route is reliable and easy to operate. The compounds have no obvious in hibitory effects againstβ-secre-tase.