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Updated: Jun 13, 2025

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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
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设计,合成和生物活性评价新型的imidazo[5,1-b]thiazole衍生物含有pyrazole环的基于中间衍生方法的中间衍生方法的设计,合成和生物活性评估
Meng Li1, Shixuan Liu1, Lei Qi1
1College of Materials and Chemistry and School of Plant Protection, Anhui Agricultural University, Hefei, China.
Pest management science
|March 4, 2025
概括
新的pyrazole imidazo[5,1-b]thiazole衍生物被合成并测试其抗真菌活性. 化合物18f显示出对Sclerotinia sclerotiorum具有较低毒性的强效,显示出作为新型真菌杀菌剂候选人的承诺.
科学领域:
- 农业化学科学 农业化学科学
- 药用化学 医学化学
- 有机合成 有机合成
背景情况:
- 中间衍生增强农药开发的成功,并降低成本.
- 合成了pyrazole imidazo[5,1-b]thiazole衍生物以修改 imine 骨架.
- 之前的研究表明,相关化合物具有良好的抗真菌活性.
研究的目的:
- 为了合成新型的pyrazole imidazo[5,1-b]thiazole衍生物.
- 评估这些新型化合物的抗真菌活性.
- 评估有望候选物的毒性和作用机制.
主要方法:
- 通过中间衍生物化合成新型皮拉伊米达佐[5,1-b]亚衍生物.
- 抗真菌活性测试对Sclerotinia sclerotiorum进行检测.
- 在菜叶上的体内疗效测试.
- 显微镜 (SEM,TEM) 用于研究细胞效应.
- 生物化学分析 (细胞含量泄漏,导电性,透性,ROS).
- 对斑马鱼的急性毒性测试.
主要成果:
- 化合物4f和18f表现出强烈的抗真菌活性 (EC500.98和0.95毫克L-1),与博斯卡利德 (EC500.82毫克L-1) 相似.
- 化合物18f对大麻叶和严重损坏的真菌细胞膜产生保护作用.
- 化合物18f对水生生物 (斑马鱼) 的毒性低于boscalid.
结论:
- 一种新的pyrazole imidazo[5,1-b]thiazole衍生物 (18f) 成功合成并显示出强大的抗真菌活性.
- 化合物18f具有低毒性,对真菌细胞膜具有显著的有害作用.
- 这种化合物代表了一种新型抗真菌农药的有希望的候选者,为未来的真菌杀菌剂开发提供了一个参考.
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