1,4-戊二烯-3-酮肟酯类化合物的合成及生物活性
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国家自然科学基金(No.21462012);贵州省优秀青年科技人才培养对象专项资金(黔科合人字(2015)35号);贵州大学研究生创新基金(No.2016076)资助项目。


Synthesis and Biological Activities of Penta-1,4-diene-3-one Oxime Ester Derivatives
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    摘要:

    以单羰基姜黄素衍生物为先导,将具有优良生物活性的肟酯基团与1,4-戊二烯-3-酮结构有机结合,设计合成了11个含肟酯结构的1,4-戊二烯-3-酮类化合物,其结构经红外光谱、核磁共振波谱、液相质谱和元素分析确证。初步生物活性测试结果表明:在质量浓度为500 mg/L时,化合物Va对烟草花叶病毒(TMV)治疗活性为61.3%,与其对照药剂宁南霉素(64.6%)相当;化合物Ve对TMV的治疗活性为91.2%,与对照药剂宁南霉素(97.3%)相当。在药剂浓度为50 mg/L时,化合物Vf对小麦赤霉病菌、水稻纹枯病菌和苹果腐烂病菌具有中等程度的抑制活性,其抑制率分别为48.1%、56.5%和66.1%。在药剂浓度为100 mg/L时,化合物Vi对小菜蛾和蚜虫具有一定程度的触杀活性,其抑制率分别为61.5%和42.4%。以上活性数据表明:1,4-戊二烯-3-酮肟酯类化合物具有一定的抗植物病毒、抑菌和杀虫活性,在其结构基础上进行适当的改造,有望得到具有良好生物活性的化合物。

    Abstract:

    A series of novel penta-1,4-diene-3-one oxime ester derivatives, which are confirm by IR, NMR, ESI-MS and elemental analysis, were synthesized via the method of combing the oxime esters groups and penta-1,4-diene-3-ones in one molecules. The results of anti-virus bioassays indicated that the curative activity of the title compounds Va against tobacco mosaic virus (TMV) was 61.3%, and the inactivition activity of the title compound Ve against TMV was 91.3%, which were comparable with the commercial agent Ningnanmycin (64.6% and 97.3%, respectively) at 500 μg/mL. Meanwhile, the title compound Vf showed moderate fungicidal activities against G. zeae, F. oxysporum and C. mandshurica at 50 μg/mL, with the inhibition rates reached respectively 48.1%, 56.5% and 66.1%. Furthermore, the title compound Vi exhibited certain insecticidal activity against P. xylostella and A. craccivora at 100 μg/mL, with the inhibition rates reached respectively 61.5% and 42.4%. These bioassys indicates that the penta-1,4-diene-3-one oxime esters has certain antiviral, fungicidal and insecticidal activities, and that some compounds with potent biological activities might be obtained via the structural modification based on the penta-1,4-diene-3-one oxime esters.

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夏丽娟.1,4-戊二烯-3-酮肟酯类化合物的合成及生物活性[J].精细化工,2017,34(7):

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  • 收稿日期:2016-11-08
  • 最后修改日期:2017-02-21
  • 录用日期:2017-03-06
  • 在线发布日期: 2017-06-02
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