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通过合理的碳-生物异构体替代策略识别了含有的新型酸性酸衍生物

Cong Zhou¹, Zhong Li¹, Xuhong Qian^1,2

¹Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.

Journal of agricultural and food chemistry

|September 18, 2023

概括

研究人员开发了新型含的pyrazolyl acrylonitriles用于虫控制. 化合物A25表现出优异的虫杀菌活性,性能优于现有的商业选择,并显示出增强的酶抑制.

科学领域:

农业化学农业化学
有机化学有机化学
虫害管理虫害管理虫害管理

背景情况:

植物虫对作物产量构成重大威胁.
开发具有更高效率的新型虫杀虫剂对于可持续农业至关重要.
现有的虫杀虫剂面临着耐药性和环境影响的挑战.

研究的目的:

设计和合成含有的新型pyrazolyl烯酸.
评估这些新化合物对植物虫的杀虫活性.
为了研究分子水平的作用机制.

主要方法:

合并碳-生物异构体替代策略的合理设计.
对于pyrazolyl acrylonitrile衍生物的新型合成方法.
毒生物测试以确定LC50值.
对糖酸脱酶 (SDH) 的酶抑制试验.
分子对接研究以阐明结合相互作用.

主要成果:

发现了一种具有强烈虫杀菌活性的A25化合物 (LC50 = 0.062 mg/L).
化合物A25的强度分别高于cyenopyrafen和cyetpyrafen的2.3倍和1.9倍.
与烯代谢产物相比,A25的活性成分M1对Tetranychus cinnabarinus SDH的IC50值高出两倍.
分子对接揭示了活性代谢物和对应物与SDH残留物的关键相互作用 (H键,-π).

结论:

含的pyrazolyl acrylonitriles代表了一个有前途的新类型的虫杀虫剂.
化合物A25显示出有效控制虫的显著潜力.
这些发现提供了对结构-活性关系和作用机制的见解,以改进杀剂设计.

关键词:

碳-生物异构体替代物复杂II结合部位结合部位计算建模计算建模烯 (cyenopyrafen) 是一种天然.赛特皮拉芬 (cyetpyrafen) 是一种天然的药物.这是一种pyrazolyl acrylonitrile 乙化物.结构结构活动关系关系

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