State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Guizhou University, Guiyang, China.
Pest Manag Sci. 2017 Oct;73(10):2079-2089. doi: 10.1002/ps.4579. Epub 2017 May 22.
Ferulic acid and quinazoline derivatives possess good antiviral activities. In order to develop novel compounds with high antiviral activities, a series of ferulic acid ester derivatives containing quinazoline were synthesized and evaluated for their antiviral activities.
Bioassays indicated that some of the compounds exhibited good antiviral activities in vivo against tobacco mosaic virus (TMV) and cucumber mosaic virus (CMV). One of the compounds demonstrated significant curative and protective activities against TMV and CMV, with EC values of 162.14, 114.61 and 255.49, 138.81 mg L , respectively, better than those of ningnanmycin (324.51, 168.84 and 373.88, 272.70 mg L ). The values of q and r for comparative molecular field analysis and comparative molecular similarity index analysis in the TMV (0.508, 0.663 and 0.992, 0.930) and CMV (0.530, 0.626 and 0.997, 0.981) models presented good predictive abilities.
Some of the title compounds demonstrated good antiviral activities. Three-dimensional quantitative structure-activity relationship models revealed that the antiviral activities depend on steric and electrostatic properties. These results could provide significant structural insights for the design of highly active ferulic acid derivatives. © 2017 Society of Chemical Industry.
阿魏酸和喹唑啉衍生物具有良好的抗病毒活性。为了开发具有高抗病毒活性的新型化合物，合成了一系列含有喹唑啉的阿魏酸酯衍生物，并对其抗病毒活性进行了评价。
生物测定表明，一些化合物在体内对烟草花叶病毒（TMV）和黄瓜花叶病毒（CMV）具有良好的抗病毒活性。其中一种化合物对 TMV 和 CMV 表现出显著的治疗和保护活性，EC 值分别为 162.14、114.61 和 255.49、138.81 mg·L ，优于宁南霉素（324.51、168.84 和 373.88、272.70 mg·L ）。TMV（0.508、0.663 和 0.992、0.930）和 CMV（0.530、0.626 和 0.997、0.981）模型中比较分子场分析和比较分子相似性指数分析的 q 和 r 值均具有良好的预测能力。
标题化合物中的一些具有良好的抗病毒活性。三维定量构效关系模型表明，抗病毒活性取决于立体和静电性质。这些结果可为设计高活性阿魏酸衍生物提供重要的结构见解。 © 2017 化学工业协会。
