设计,合成和杀虫剂评价使用结合烯的新尼古丁类药物
Yiping Wang1, Xiao Zhang1, Yijin Kong1
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
|July 20, 2023
概括
合成了新型的尼类药物类似物,并对杀虫活性进行了测试. 化合物A3和A12对Myzus persicae的疗效与伊米达克洛普里德相当,在水中稳定性更强.
科学领域:
- 农业化学 农业化学
- 有机化学 有机化学
- 杀虫剂开发 杀虫剂开发
背景情况:
- 类杀虫剂针对昆虫的尼古丁乙胆受体 (nAChRs) 进行害虫控制.
- 开发新的类似物对于有效和可持续的害虫管理至关重要.
研究的目的:
- 为了合成一种新型的氨基类类似物,其中包含一个结合的二烯分子.
- 评估这些新化合物的杀虫活性和稳定性.
主要方法:
- 合成新类类药物的类似物.
- 对Myzus persicae进行生物测试以确定LC50值.
- 密度函数理论 (DFT) 的计算和与Lymnaea stagnalis AChBP的分子对接.
- 水解实验,以评估水中的稳定性.
主要成果:
- 化合物A3和A12对Myzus persicae的LC50值分别为1.26和1.24毫克/升.
- 这些活动与参考杀虫剂伊米达克洛普里德 (LC50 = 0.78 mg/L) 相似.
- DFT和分子对接表明A3和A12与昆虫nAChRs的良好相互作用,并且证实了增强的水解稳定性.
结论:
- 合成的新烟类类似物,特别是A3和A12,显示出显著的杀虫潜力.
- 这些化合物为开发具有更高稳定性的新害虫防治剂提供了有希望的基础.
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