小说5- ((三甲基) -1,2,4-oxadiazole-based Pyrimidin-4-ether 控制生疾病的酸酶抑制剂:设计,合成,活性和结构-活性关系
Xing-Hai Liu1, Chen-Hao Fu1,2, Jian Wang1,2
1College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014, China.
Journal of agricultural and food chemistry
|February 12, 2025
概括
新的三甲基洛克沙迪 (TFMO) 杀菌剂在作物中显示出极好的防作用. 化合物XII6有效地对抗像*Puccinia pachyrhizi*和*Puccinia rubigo*这样具有低毒性的病原体,为现有治疗提供了一个有希望的替代方案.
科学领域:
- 农业化学 农业化学
- 植物病理学 植物病理学
- 药用化学 医学化学
背景情况:
- 由植物病原体引起的生疾病显著降低了作物和水果产量.
- 三甲基洛克沙迪亚 (TFMO) 化合物是已知的基因素脱乙酶抑制剂 (HDAC).
研究的目的:
- 设计和合成基于TFMO的新型pyrimidin-4-ether衍生物作为潜在的杀菌剂.
- 评估这些化合物对关键植物生病原体的有效性和安全性.
主要方法:
- 合成了一系列基于5- ((trifluoromethyl) -1,2,4-oxadiazole (TFMO) 的胺-4-衍生物.
- 针对 *Puccinia sorghi*, *Phakopsora pachyrhizi* 和 *Puccinia rubigo* 的反信任生物测试.
- 酶抑制测定,急性毒性测试和结构-活性关系 (SAR) 分析.
主要成果:
- 几种合成的TFMO衍生物对植物生病原体表现出极好的活性.
- 化合物XII6与阿佐克西斯特罗宾相比,对*P. pachyrhizi* (50%在0.780 mg/L下) 的控制能力更强.
- 实地试验证实了化合物XII6对*P. rubigo* (116g/ha) 的有效性,具有低急性毒性.
- 化合物XII6被确定为一种强效,非选择性的HDAC抑制剂.
结论:
- 该研究成功开发了基于TFMO的新型胺-4-衍生物,具有针对生疾病的显著杀菌特性.
- 化合物XII6是农业中生管理的高效和低毒性真菌杀菌剂候选物.
- 为了增强农业应用,需要进一步优化化合物XII6.
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