State Key Laboratory of Green Pesticide, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for R&D of Fine Chemicals of Guizhou University, Guiyang 550025, China.
J Agric Food Chem. 2024 Aug 21;72(33):18378-18390. doi: 10.1021/acs.jafc.4c02889. Epub 2024 Aug 7.
Resistant weeds severely threaten crop yields as they compete with crops for resources required for survival. Trifludimoxazin, a protoporphyrinogen IX oxidase (PPO) inhibitor, can effectively control resistant weeds. However, its crop safety record is unsatisfactory. Consequently, a scaffold-hopping strategy is employed in this study to develop a series of new triazinone derivatives featuring an amide structure. Most compounds depicted excellent herbicidal activity across a broad spectrum at 37.5-150 g ai/ha, among which ()- was equivalent to flumioxazin. ()- demonstrated significant crop tolerance to rice and wheat, even at 150 g ai/ha. ()- exhibited superior pharmacokinetic features compared to flumioxazin and trifludimoxazin. This was depicted by the absorption, distribution, metabolism, excretion, and toxicity predictions. Notably, proteomics-based analysis was applied for the first time to investigate variations among plant proteins before and after herbicide application, shedding light on the conservative and divergent roles of PPO.
抗药性杂草严重威胁作物产量，因为它们与作物竞争生存所需的资源。三氟啶磺隆，一种原卟啉原氧化酶（PPO）抑制剂，可以有效地控制抗药性杂草。然而，其在作物安全方面的记录并不令人满意。因此，本研究采用了一种支架跳跃策略，开发了一系列具有酰胺结构的新型三嗪酮衍生物。大多数化合物在 37.5-150 g ai/ha 之间表现出广谱高效的除草活性，其中 ()-与氟噻草胺相当。()-对水稻和小麦表现出显著的作物耐受性，即使在 150 g ai/ha 的剂量下也是如此。()-与氟噻草胺和三氟啶磺隆相比，表现出更好的药代动力学特征。这是通过吸收、分布、代谢、排泄和毒性预测来描述的。值得注意的是，基于蛋白质组学的分析首次应用于研究除草剂施用前后植物蛋白的变化，揭示了 PPO 的保守和分歧作用。
