| 陈丽娟,李普,王晓斌,阮祥辉,薛伟.化学通报,2017,80(12):1156-1159. |
| 1,4-戊二烯-3-酮肟醚类化合物的合成及生物活性 |
| Synthesis and biological activities of penta-1,4-diene-3-one Oxime ether Derivatives |
| 投稿时间：2017-05-20 修订日期：2017-07-06 |
| DOI： |
| 中文关键词: 1,4-戊二烯-3-酮 肟醚 抗病毒活性 烟草花叶病毒 |
| 英文关键词:penta-1,4-diene-3-one, oxime ether, antiviral activity, tobacco mosaic virus |
| 基金项目:国家自然科学基金项目（21462012），贵州省优秀青年科技人才培养对象专项资金(201535)和贵州大学研究生创新基金(No.2017060) |
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| 中文摘要: |
| 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：在药剂质量浓度为500 mg/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 %,优于对照药剂病毒唑(87.9%)。研究结果表明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先导优化,有望得到具有良好抗植物病毒活性的先导化合物。 |
| 英文摘要: |
| Seven novel penta-1,4-diene-3-one oxime ether derivatives, which were confirmed by IR, 1H NMR, 13C NMR and ESI-MS, were synthesized by converting carbonyl groups in the 1,4-pentadien-3-ones to an oxime ether groups. Antiviral bioassays at 500 mg/L indicated that compounds 4c, 4f,and 4g exhibited better curative activity against tobacco mosaic virus (TMV) (49.6, 53.6 and 47.4%, respectively) than ribavirin (45.2%); that protective activities of compounds 4b, 4c, 4f and 4g against TMV were respectively 57.2, 58.4, 58.9 and 59.0%, which were lower than that of ribavirin (61.8%); and that inactivition activities of compounds 4a, 4b, 4c and 4g against TMV were respectively 95.5, 92.6, 95.0 and 89.5 %, which were superior to that of ribavirin (87.9%). These results indicated that penta-1,4-diene-3-one oxime ether derivatives had good inhibitory effect against plant virus, and that some compounds with potent anti-plant viral activities can be obtain based on properly modifications on structures of penta-1,4-diene-3-one oxime ethers. |
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