Huang Guang-Ying, Cui Can, Wang Zhi-Peng, Li Yong-Qiang, Xiong Li-Xia, Wang Li-Zhong, Yu Shu-Jing, Li Zheng-Ming, Zhao Wei-Guang
State Key Laboratory of Elemento-Organic Chemistry, National Pesticide Engineering Research Center (Tianjin), Nankai University, Tianjin 300071, China.
Chem Cent J. 2013 Feb 14;7(1):33. doi: 10.1186/1752-153X-7-33.
Plant viruses cause many serious plant diseases and are currently suppressed with the simultaneous use of virucides and insecticides. The use of such materials, however, increases the amounts of pollutants in the environment. To reduce environmental contaminants, virucides with insecticidal activity is an attractive option.
A series of substituted ferulic acid amide derivatives 7 and the corresponding hydrogenated ferulic acid amide derivatives 13 were synthesized and evaluated for their antiviral and insecticidal activities. The majority of the synthesized compounds exhibited good levels of antiviral activity against the tobacco mosaic virus (TMW), with compounds 7a, 7b and 7d in particular providing higher levels of protective and curative activities against TMV at 500 μg/mL than the control compound ribavirin. Furthermore, these compounds displayed good insecticidal activities against insects with piercing-sucking mouthparts, which can spread plant viruses between and within crops.
Two series of ferulic acid derivatives have been synthesized efficiently. The bioassay showed title compounds not only inhibit the plant viral infection, but also prevented the spread of plant virus by insect vectors. These findings therefore demonstrate that the ferulic acid amides represent a new template for future antiviral studies.
植物病毒会引发多种严重的植物病害，目前通过同时使用杀病毒剂和杀虫剂来抑制。然而，此类物质的使用会增加环境中的污染物含量。为减少环境污染物，具有杀虫活性的杀病毒剂是一个颇具吸引力的选择。
合成了一系列取代阿魏酸酰胺衍生物7以及相应的氢化阿魏酸酰胺衍生物13，并对其抗病毒和杀虫活性进行了评估。大多数合成化合物对烟草花叶病毒（TMV）表现出良好的抗病毒活性，尤其是化合物7a、7b和7d在500μg/mL时对TMV的保护和治疗活性高于对照化合物利巴韦林。此外，这些化合物对具有刺吸式口器的昆虫表现出良好的杀虫活性，这类昆虫会在作物间和作物内传播植物病毒。
已高效合成了两个系列的阿魏酸衍生物。生物测定表明，标题化合物不仅能抑制植物病毒感染，还能防止植物病毒通过昆虫载体传播。因此，这些发现表明阿魏酸酰胺代表了未来抗病毒研究的新模板。
