Department of Chemistry, Zhejiang University, Hangzhou 310058, China.
National Joint Local Engineering Laboratory for High-Efficient Preparation of Biopesticide, College of Forestry and Biotechnology, Zhejiang A & F University, Hangzhou 311300, China.
J Agric Food Chem. 2024 Jul 24;72(29):16140-16151. doi: 10.1021/acs.jafc.4c03891. Epub 2024 Jul 15.
Given the prevalence of the malignant weed Chinese Sprangletop ( (L.) Nees) in rice fields, the development of novel herbicides against this weed has aroused wide interest. Here, we report a novel diphenyl ether-pyrimidine hybrid, DEP-, serving as a systematic pre/postemergence herbicide candidate for broad-spectrum weed control in rice fields, specifically for . Notably, DEP- exhibits over 80% herbicidal activity against the resistant biotypes even at 37.5 g a.i./ha under greenhouse conditions and has complete control of at 150 g a.i./ha in the rice fields. We uncover that DEP- acts as a noncompetitive inhibitor of acetohydroxyacid synthase (AHAS) with an inhibition constant () of 39.4 μM. We propose that DEP- binds to AHAS in two hydrophobic-driven binding modes that differ from commercial AHAS inhibitors. Overall, these findings demonstrate that DEP- has great potential to be developed into a herbicide for control and inspire fresh concepts for novel AHAS-inhibiting herbicide design.
鉴于恶性杂草稻李氏禾在稻田中的普遍存在，开发针对这种杂草的新型除草剂引起了广泛关注。在这里，我们报告了一种新型的二苯醚-嘧啶杂合体 DEP-，可用作系统的前/后出苗除草剂候选物，用于稻田中广谱杂草控制，特别是针对 。值得注意的是，DEP-在温室条件下，即使在 37.5 g a.i./ha 的用量下，对抗性生物型也表现出超过 80%的除草活性，在稻田中，150 g a.i./ha 的用量可完全控制 。我们发现 DEP-是乙酰羟酸合酶 (AHAS) 的非竞争性抑制剂，抑制常数 () 为 39.4 μM。我们提出，DEP-以两种不同于商业 AHAS 抑制剂的疏水驱动结合模式与 AHAS 结合。总的来说，这些发现表明 DEP-有很大潜力被开发成一种用于控制 的除草剂，并为新型 AHAS 抑制性除草剂设计提供了新的概念。
