新型Isoxazoline Acylhydrazone化合物的设计,合成和杀虫活性
Yahui Li1,2, Shaochen Li2, Xue Yin2
1State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang, China.
Pest management science
|November 20, 2023
概括
新型含有乙烯基的异zoline衍生物对钻石背 (Plutella xylostella) 具有强大的杀虫活性. 化合物E3表现出与商业农药相美的异常有效性,突出了其在作物保护方面的潜力.
科学领域:
- 农业化学科学 农业化学科学
- 有机化学 有机化学
- 昆虫学 昆虫学是一门学科.
背景情况:
- 钻石背 (Plutella xylostella) 对十字类蔬菜构成重大威胁.
- 迫切需要有效的农药来保护农作物免受这种害虫的侵害.
- 这项研究的重点是开发新的杀虫剂化合物.
研究的目的:
- 合成和评估新型含有乙基部分作为潜在杀虫剂的异zoline衍生物.
- 评估这些化合物的杀虫活性对抗Plutella xylostella和其他Lepidopteran害虫.
- 研究最强效化合物的结构-活性关系和分子相互作用.
主要方法:
- 新型异黄酸衍生物的合成.
- 使用质子核磁共振 (1H NMR),碳-13核磁共振 (13C NMR) 和高分辨率质谱法 (HR-MS) 的结构阐明.
- 杀虫剂活性测定对抗Plutella xylostella,Pyrausta nubilalis和Chilos suppressalis. 这三种植物的杀虫活性测定.
- 针对GABA受体的分子对接研究和密度功能理论 (DFT) 计算.
主要成果:
- 大多数合成衍生品对Plutella.xylostella表现出杀虫活性.
- 化合物E3对Plutella xylostella (LC50 = 0.19毫克L-1) 显示出优越的活性,表现优于乙二,与流量胺胺相比.
- 化合物E3还对Pyrausta nubilalis和Chilo suppressalis.也表现出强大的活性.
- 分子对接表示E3与GABA受体活性部位形成关键相互作用 (和Pi-Pi键).
- 结构-活性关系分析发现R替代剂对杀虫剂活性至关重要.
结论:
- 伊索克萨氨酸化衍生物代表了一类有前途的杀虫剂.
- 化合物E3是一种高效的候选物,用于控制Plutella xylostella和其他Lepidopteran害虫.
- 对这些衍生物的进一步研究可能会导致新的作物保护策略.
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