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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-NMRI、R、MS谱确证;仅有化合物A5显示出较好的抗禽流感病毒活性。
Objective To design a synthetic amantadine derivative and test its anti-avian influenza virus activity. Methods Starting from adamantanecarbonyl chloride and amino acid methyl ester hydrochloride, three series of amantadine derivatives were obtained by amidation, hydrolysis and salt reaction. Using amantadine as a positive control, the anti-avian influenza virus activity of the target compounds was determined by plaque formation assay in puppies and kidney (MDCK) cell lines. RESULTS AND CONCLUSIONS A total of 20 novel compounds were reported. The structures of the target compounds were confirmed by1H-NMR1, R and MS spectra. Only compound A5 showed betteranti-avian influenza virus activity.