发现和优化可抑制乙烯基-ACP硫酶的螺旋环乳酸盐
Elisabeth Asmus1, David M Barber1, Guido Bojack1
1Research & Development, Weed Control, Division Crop Science, Bayer AG, Industriepark Höchst, Frankfurt, Germany.
Pest management science
|February 9, 2024
概括
研究人员开发了针对acyl-ACP thioesterase的新型螺旋 laktam 除草剂,以对抗抗性草杂草. 这些化合物在小麦和玉米等作物中显示出有希望的 in vivo 疗效和选择性.
科学领域:
- 农业化学科学 农业化学科学
- 有机化学 有机化学
- 农作物保护 农作物保护
背景情况:
- 控制杂草是全球农业面临的挑战,其中小分子除草剂是主要解决方案.
- 开发具有新作用模式的新型除草剂对于管理抗除草剂杂草至关重要.
- 乙-ACP硫酶抑制剂是除草剂开发的目标类.
研究的目的:
- 发现具有除草剂活性的新型化学实体.
- 为了研究螺旋环酸-ACP硫酶抑制剂.
- 识别用于控制耐药草杂草的结构.
主要方法:
- 利用X射线共晶结构和分子建模.
- 采用了脚手架跳跃和同位素概念来优化线.
- 进行了体内试验和温室试验,以评估疗效和选择性.
主要成果:
- 鉴定了基于螺旋的新型结构,具有高目标亲和力.
- 在体内表现出有希望的活性,对抗关键草杂草.
- 在小麦和玉米中实现了草杂草的有效前期控制,在小麦和玉米中具有部分选择性.
结论:
- 开发了新型除草剂结构,具有螺旋环乳酸核.
- 这些化合物表现出强大的乙-ACP化酶抑制和强烈的除草剂活性.
- 显示对抗耐药草杂草的有效性,与商业标准相比.
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