发现含有二乙烯碎片的thiazole-5-carboxamide衍生物作为潜在的糖酸脱酶抑制剂
Zhongzhong Yan1,2,3, Yujie Wang1,2, Yanhua Jiang1,2
1Key Laboratory of Industrial Dust Prevention and Control & Occupational Health and Safety, Ministry of Education, Anhui University of Science and Technology, Huainan 232001, PR China.
Journal of agricultural and food chemistry
|October 7, 2025
概括
新的 thiazole-5-carboxamide 杀菌剂与二乙醇碎片显示出强大的抗真菌活性. 化合物IIIe有效控制米病,为作物保护提供了一个有希望的替代品.
科学领域:
- 农业化学 农业化学
- 菌类学 菌类学是指菌类学.
- 有机合成 有机合成
背景情况:
- 酸脱酶抑制剂 (SDHI) 对于作物保护至关重要.
- 在SDHI中用二乙醇碎片取代双是开发新型真菌杀菌剂的战略.
研究的目的:
- 设计和评估含有烯酸乙碎片抗真菌活性的新型 thiazole-5-carboxamide 衍生物.
- 确定用于农业应用的强效SDHI杀菌剂.
主要方法:
- 对45种提亚-5-碳胺衍生物的合成和抗真菌评估,针对关键的植物病原体.
- 对有前途的化合物的体外和体内疗效测试,包括化合物IIIe.
- 作用机制研究涉及SDH抑制,呼吸和线粒体功能.
主要成果:
- 与商用杀菌剂相比,化合物IIIe在体外对*Rhizoctonia solani* (EC50 = 0.009 mg/L) 具有更高的活性.
- 化合物IIIe在独立的叶子和实验中显示出对控制大米病的高疗效.
- 机制研究证实了IIIe化合物作为SDHI的作用,向真菌呼吸.
结论:
- 设计的含烯乙烯的 thiazole-5-carboxamides 是一种有前途的新型 SDHI 杀菌剂.
- 化合物IIIe显示出作为一个具有成本效益和高效的农业用途的真菌杀菌剂的巨大潜力.
- 这项研究为SDHI杀菌剂的结构优化提供了宝贵的见解.
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