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新型含二硫缩醛部分的喹喔啉衍生物的合成、抗马铃薯 Y 病毒活性及作用机制。

Synthesis, Anti-Potato Virus Y Activities, and Interaction Mechanisms of Novel Quinoxaline Derivatives Bearing Dithioacetal Moiety.

机构信息

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang, Guizhou 550025, People's Republic of China.

出版信息

J Agric Food Chem. 2022 Jun 15;70(23):7029-7038. doi: 10.1021/acs.jafc.2c01898. Epub 2022 Jun 1.

Abstract

Quinoxaline and its derivatives are important functional molecules with a broad range of applications. Disclosed here is a design and synthesis of a series of novel quinoxaline derivatives containing dithioacetal moieties as well as their antiviral activities against potato virus Y (PVY). The compound was developed on the basis of the three-dimensional quantitative structure-activity relationship. The anti-PVY activity test showed that the half maximal effective concentration of the anti-PVY protective activity of compound is 197 μg/mL, which was better than the control agents ningnanmycin (423 μg/mL) and xiangcaoliusuobingmi (281 μg/mL). Significantly, compound can increase defense enzyme activity and chlorophyll content, promote photosynthesis by accelerating carbon fixation in tobacco, and further improve plant disease resistance. All of these results suggest that compound could be employed as a lead compound for novel PVY inhibitor discovery.

摘要

噁二嗪及其衍生物是一类重要的功能分子,具有广泛的应用。本研究设计并合成了一系列含有二硫缩醛片段的噁二嗪衍生物,并对其抗马铃薯 Y 病毒(PVY)的活性进行了评价。基于三维定量构效关系,设计合成了化合物 。抗 PVY 活性测试表明,化合物 的抗 PVY 保护活性的半数有效浓度(EC50)为 197μg/mL,优于对照药剂宁南霉素(423μg/mL)和香菇多糖(281μg/mL)。值得注意的是,化合物 能够提高防御酶活性和叶绿素含量,通过加速烟草的碳固定促进光合作用,从而进一步提高植物的抗病性。这些结果表明,化合物 可能成为新型 PVY 抑制剂发现的先导化合物。

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