制备,特征和生物活性的propargite立体同位素的制备,特征和生物活性
Yingshuai Liu1,2, Guozhu Sheng2, Baohong Liu2
1Shenyang Agricultural University, Plant Protection College, Shenyang, China.
Pest management science
|June 20, 2025
概括
奇拉性显著影响农药的有效性. 这项研究描述了propargite的立体异构体,揭示了P (1S,2S) 作为一种强有力的杀剂候选物,尽管需要成本有效的合成.
科学领域:
- 农业化学科学 农业化学科学
- 立体化学是一种立体化学.
- 有机化学 有机化学
背景情况:
- 性对于杀虫剂的有效性至关重要,它影响生物活性,选择性和环境影响.
- 1963年首次制备的商业虫杀虫剂普罗帕吉特的异构成分仍然定义不佳.
- 之前的研究引用了propargite I和II,没有明确的结构定义,需要对其立体同位素进行研究.
研究的目的:
- 准备和结构性表征各种propargite立体同位素.
- 评估不同propargite异构体的虫杀菌活性和作物安全性.
- 为了确定未来发展的有前途的性虫杀虫剂.
主要方法:
- 合成和结构性表征八个目标propargite立体异构体.
- 制备P (trans) 和P (cis) 等混合物,以及P (1S,2S) 和P (1R,2R) 等特定异构体.
- 使用LC50值对虫杀虫活性的评估,以及对牛苗的作物安全性的评估.
主要成果:
- 与P (1R,2R) (LC50 = 62.84 mg L-1) 相比,P (1S,2S) 异构体表现出显著更高的糖性活性 (LC50 = 17.83 mg L-1).
- 在跨立体异构体中,P (trans) -1表现出最强的活性 (LC50 = 13.00 mg L-1).
- P (trans) 和P (cis) 异构体表现出可比的杀性活性 (LC50 ≈ 29-32 mg L-1),所有测试的异构体在牛苗上表现出相当的作物安全性.
结论:
- 由于其高疗效,propargite立体同位素P (1S,2S) 显示出作为一种性虫杀菌剂的潜力.
- 为了使其具有商业可行性,需要对P (1S,2S) 具有成本效益的合成方法进行进一步研究.
- 这项研究澄清了propargite立体同位素的结构和活性关系,有助于开发更有效的农业化学品.
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