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本研究基于苯甲酸衍生物类神经氨酸酶抑制剂的结构,依据最新报道的构效关系设计了新的先导化合物 L,并合成4个未见文献报道的苯甲酸衍生物类神经氨酸酶抑制剂 ( Ⅰ~Ⅳ )。活性测试选用流感病毒菌株 H_3N_2( California/04)、H_1N_1(California/99) 和 B(Shanghai/02)。结果显示,化合物Ⅰ~Ⅳ均具有良好的神经氨酸酶抑制作用,含环状分支的Ⅱ活性最佳。
In this study, based on the structure of benzoic acid derivative neuraminidase inhibitors, a new lead compound L was designed according to the recently reported structure-activity relationship and four benzoic acid derivative neuraminidase Inhibitors (Ⅰ ~ Ⅳ). Influenza virus strains H_3N_2 (California / 04), H_1N_1 (California / 99) and B (Shanghai / 02) were selected for the activity test. The results showed that all compounds Ⅰ ~ Ⅳ had good neuraminidase inhibitory activity, and the activity of Ⅱ with ring branch was the best.