设计,合成和新型含有Pyrazole环的Paeonol衍生物的抗Oomycete和抗真菌活动
Yibo Liu1, Yuee Tian1, Hong Peng2
1Laboratory of Pesticidal Design & Synthesis, Department of Plant Protection, College of Horticultrue and Plant Protection, Henan University of Science and Technology, Luoyang 471023, China.
Journal of agricultural and food chemistry
|April 11, 2025
概括
研究人员用Pyrazole环合成了25种paeonol衍生物,以发现新的天然杀菌剂. 九种衍生物显示出对Phytophthora capsici有前途的抗虫活性,六种显示出对Fusarium graminearum的抗真菌活性.
科学领域:
- 自然产品化学 自然产品化学
- 药用化学 医学化学
- 农业科学 农业科学
背景情况:
- 培醇是从培根树皮中提取的,是中国传统医学的关键成分.
- 需要基于生物理性的天然产品的杀菌剂来对抗农业疾病.
- 皮拉衍生物因其潜在的生物活性而被探索.
研究的目的:
- 设计和合成包含Pyrazole环的新型Paeonol衍生物.
- 评估这些新化合物对关键植物病原体的抗虫和抗真菌活性.
- 研究结构-活性关系,以开发有效的植物作物保护剂.
主要方法:
- 合成了25种含有pyrazole部分的paeonol衍生物 (5a-y化合物).
- 使用NMR光谱,HRMS和点分析进行结构性表征.
- 通过单晶X射线衍射来确定所选化合物的立体化学配置.
- 生物测试以评估对*Phytophthora capsici*和对*Fusarium graminearum**的抗真菌活性.
主要成果:
- 九种醇衍生物 (5b-d, 5f, 5g, 5r, 5s, 5u, 5w) 对 *P. capsici* 具有显著的抗虫活性,EC50值在22.1至34.5mg/L之间.
- 六种衍生品 (5g,5k,5m,5t,5w,5x) 对 *F. graminearum* 显示出有前途的抗真菌活性,EC50值在38.2至86.0 mg/L之间.
- 在体内测试证实了测试化合物对*P. capsici*的保护作用.
结论:
- 合成的帕埃诺-皮拉衍生物显示出作为新型植物性杀菌剂的潜力.
- 该研究确定了针对虫和真菌植物病原体具有显著活性的特定化合物.
- 这些发现为未来开发用于农业作物保护的醇衍生物提供了基础.
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