目的研究新型作用于150位活性口袋的含芳基甲酰胺类的神经氨酸酶抑制剂。方法以奥司他韦为先导化合物,结合近年来报道的作用于150位活性口袋的化合物的结构特征,设计了9个未见文献报道的含芳基甲酰胺结构的化合物,采用半合成的方法完成了目标化合物的合成,进行了初步药理活性测试。结果与结论化合物2d表现了较强的抑制活性,其他化合物表现中等强度的酶抑制活性。 Aim To study a novel aryl formamidine neuraminidase inhibitor that acts on 150 active pockets. Methods Using oseltamivir as the lead compound and combining with the structural characteristics of the compounds reported in recent 150 years in the active pocket of 150, nine novel compounds with aryl formamide structures were designed and synthesized by semi-synthetic method The synthesis of the target compound was completed and a preliminary pharmacological activity test was carried out. RESULTS AND CONCLUSION Compound 2d showed strong inhibitory activity and other compounds exhibited moderate activity of enzyme inhibitory activity.