含喹唑啉(喹唑啉酮)苯醚取代-1,4-戊二烯-3-酮衍生物合成与抗植物病毒活性

Plant virus disease is a worldwide important threat to agriculture, it poses a difficult problem for us to study the prevention and control of plant viral diseases.Based on these important and difficult challenges and our group carried out intensive research on discovering novel antiviral lead structure and agent for plant. Used Curcumin analogues,1,4-pentadien-3-one as lead compound, a series of novel (1E,4E)-1-(substituted-phenyl)-5-[(4-(3H)-quinazolinone)-3- methoxyl]phenyl-penta-1,4-dien-3-one,(1E,4E)-1-(substituted-phenyl)-5-[(4-(3H)-quinazolinone-3-methylthiophenyl-penta-1,4-dien-3-one,(1E,4E)-1-(substituted- phenyl)-5-(2-(quinazolin-4-yloxyl)phenyl)penta-1,4-dien-3-one and (1E,4E)-1- (substituted-phenyl)-5-[(2-quinazolin-4-ylthio)phenyl]-penta-1,4-dien-3-one will been designed and synthesized with quinazoline heterocyclic bioactive groups introduced into the targeted molecules. The novel target compounds compounds are synthesized and tested their bioactivity against CMV and TMV. On the basis of high effect new compounds, more series of derivatives will been synthesized and bioassayed. Preliminary research on their action mechanism will be also carried out. SAR research is also taken to optimize their structures. From this research new lead compound with higher bioactivity is expected. Further field test is conducted and the toxicity of the high active compounds should been evaluated.

植物病毒病害对全球农业造成严重威胁，有效防控植物病毒病害仍是重大难题,基于其防控重要性和困难挑战性,本课题以姜黄素类似物1,4-戊二烯酮为先导，引入喹唑啉(酮)杂环活性基团，设计与合成(1E, 4E)-1-(取代苯基)-5-[(4-(3H)-喹唑啉酮)-3-甲氧基]苯基-1,4-戊二烯-3-酮类、(1E, 4E)-1-(取代苯基)-5-[(4-(3H)-喹唑啉酮)-3-甲硫基]苯基-1,4-戊二烯-3-酮类、 (1E, 4E)-1-(取代苯基)5-(2-喹唑啉-4-基氧基)苯基)-1,4-戊二烯-3-酮类衍生物，测试新化合物抗病毒生物活性；在高活性化合物基础上，进一步扩大系列新化合物的合成数量,测定它们的抗病毒生物活性，寻找农药新先导结构，开展化合物作用机制研究；开展构效关系研究，优化结构，预期筛选活性更高先导化合物或新抗病毒剂，开展田间小区药效试验和急性毒性试验.

本课题以姜黄素类似物1,4-戊二烯酮为先导，引入喹唑啉(酮)杂环活性基团，设计与合成(1E, 4E)-1-(取代苯基)-5-[(4-(3H)-喹唑啉酮)-3-甲氧基]苯基-1,4-戊二烯-3-酮类、(1E, 4E)-1-(取代苯基)-5-[(4-(3H)-喹唑啉酮)-3-甲硫基]苯基-1,4-戊二烯-3-酮类、 (1E, 4E)-1-(取代苯基)5-(2-喹唑啉-4-基氧基)苯基)-1,4-戊二烯-3-酮类等九类衍生物，测试新化合物抗病毒生物活性；在高活性化合物基础上，进一步扩大系列新化合物的合成数量,测定它们的抗病毒生物活性，寻找农药新先导结构，开展化合物作用机制研究；开展构效关系研究，优化结构，共合成出 189 个以上新化合物, 发现了4个高活性化合物,发表 SCI收录论文 16 篇；培养硕士研究生 6 名、博士研究生 2 名；申请国家发明专利 4 项, 授权专利7 项。

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