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将1,4-戊二烯-3-酮结构中的羰基转变为肟醚基团,合成了7个1,4-戊二烯-3-酮肟醚类化合物,其结构经1H NMR、13C NMR、IR和ESI-MS表征。生物活性测试结果表明,在药剂浓度为500mg/L时,化合物4c、4f和4g对烟草花叶病毒(TMV)在治疗作用方面的抑制率为49.6%、53.6%和47.4%,与病毒唑(45.2%)相当;化合物4b、4c、4f和4g对TMV在保护作用方面的抑制率分别为57.2%、58.4%、58.9%和59.0%,稍低于病毒唑(61.8%);化合物4a、4b、4c和4g对TMV在钝化作用方面的抑制率分别为95.5%、92.6%、95.0%和89.5%,优于对照药病毒唑(87.9%)。这些结果表明,1,4-戊二烯-3-酮肟醚类化合物对植物病毒表现有良好抑制作用,在其结构基础上进行适当的优化,有望得到具有良好抗植物病毒活性的先导化合物。
The 1,4-pentadiene-3-one carbonyl structure was converted to an oxime ether group. Seven 1,4-pentadiene-3-oxime ether compounds were synthesized and their structures were confirmed by 1H NMR, 13C NMR, IR and ESI-MS. The bioassay results showed that the inhibitory rates of compounds 4c, 4f and 4g against tobacco mosaic virus (TMV) were 49.6%, 53.6% and 47.4%, respectively, at doses of 500 mg / L, 45.2%). The inhibition rates of compounds 4b, 4c, 4f and 4g on the protective effect of TMV were 57.2%, 58.4%, 58.9% and 59.0% respectively, slightly lower than that of ribavirin (61.8%); Compounds 4a, 4b , 4c and 4g on the passivation of TMV inhibition rates were 95.5%, 92.6%, 95.0% and 89.5%, respectively, better than the control drug ribavirin (87.9%). These results indicate that 1, 4-pentadiene-3-ketoxime ethers have a good inhibitory effect on plant virus performance. Based on their structural optimization, it is expected that lead compounds with good anti-plant virus activity will be obtained.