金刚烷胺衍生物的设计、合成及其抗禽流感病毒活性

目的 设计合成金刚烷胺衍生物并对其进行抗禽流感病毒活性测试。方法 以金刚烷甲酰氯和氨基酸甲酯盐酸盐为起始原料经酰胺化、水解、成盐等反应依次得到3个系列金刚烷胺衍生物。以金刚烷胺为阳性对照，采用幼犬肾（MDCK）细胞系噬斑形成实验测定目标化合物的抗禽流感病毒活性。结果与结论 共合成了20 个未见报道的新化合物，目标化合物的结构均经¹H-NMR、IR、MS 谱确证；仅有化合物 A₅ 显示出较好的抗禽流感病毒活性。

Design,synthesis and anti-H5N1 activities of amantadine derivatives

Based on the good antiviral activity of lead compound amantadine,in order to study on the influence of the different groups on adamantane scaffold on the anti-H5N1 activity,twenty novel amantadine derivatives were designed and synthesized.The synthetic routes of the target compounds were as follows:series A(A1-A10) were obtained from 1-adamantanecarbonyl chloride by reaction with amino acid methyl ester hydrochloride;series B(B1-B5) were obtained from amantadine derivatives series A by acid-hydrolysis;serie...