蔬菜病毒病害种类多，危害大，防治困难，对农业造成严重威胁，且防治药剂利用率低，因此寻求高效、低毒和利用率高的的抗病毒药剂具有重要意义。本申请课题采用活性亚结构拼接策略，以天然产物喹唑啉酮为母体与不同糖为原料，经“点击”反应，巧妙合成系列结构新颖的、具有韧皮部输导性和抗蔬菜病毒活性的双功能喹唑啉酮三唑糖苷化合物，并测试其对3种蔬菜病毒TMV、CMV和PVY的保护、钝化活性。结合活性与结构关系，构建3D-QSAR模型，优化设计与合成更高活性的抗病毒化合物。在高活性化合物基础上，开展有助于提高农药利用率的韧皮部输导性研究。申请项目的成功开展为高效、低毒、环境友好的抗蔬菜病毒药剂研发提供新结构，为提高农药利用率的研究提供新思路，有助于发现具有更高活性抗蔬菜病毒病药剂的先导结构。

There are many kinds of vegetable virus diseases, which are harmful, difficult to prevent and cure, and pose a serious threat to agriculture. Meanwhile, the utilization ratio of the pesticides is low, so it is great significant to seek for antiviral agents with high efficiency, low toxicity and high utilization rate. In this program, the natural product quinazolinone was used as the parent compound and different sugars were used as raw materials. A series of quinazolinone glycosides containing 1,2,3-triazolyl were subtly synthesized via Click Chemistry. The protection and inactivation activities of these compounds against tobacco mosaic virus, cucumber mosaic virus and potato Y virus were tested by in vivo, and the relationship between antivirus activity and structure was also studied. A 3D-QSAR model was constructed to optimize structures in order to design more active antiviral compounds. On the basis of high antivirus activity, phloem mobility were carried out in order to obtain the compounds with high utilization ratio. The successful development of the project can provide a new structure with efficient, low toxic and environmentally friendly antiviral agents for vegetables, provide a new idea for improving the utilization rate of pesticides and help to find the leading structure of anti-vegetable virus agents with higher activity.