College of Plant Protection, Hebei Agricultural University, Baoding, Hebei 071001, People's Republic of China.
College of Science, Hebei Agricultural University, Baoding, Hebei 071001, People's Republic of China.
J Agric Food Chem. 2021 Oct 13;69(40):11773-11780. doi: 10.1021/acs.jafc.1c01804. Epub 2021 Sep 29.
Transketolase (TK) represents a potential target for novel herbicide development. To discover novel TK inhibitors with potency against resistant weeds, 36 thioether compounds containing 1,2,4-triazole Schiff bases were designed and synthesized for herbicidal activity evaluation. The results demonstrated that compounds and provided excellent weed control with inhibition of over 90% against the tested weeds, even at concentrations as low as 100 mg/L . In addition, compounds and exhibited higher postemergence herbicidal activity than all of the positive controls against the tested weeds at 50-90 g [active ingredient (ai)]/ha in a greenhouse, while being safe for crops of maize and wheat at 90 g (ai)/ha. Fluorescent binding experiments of TK indicated that compounds and had strong TK inhibitory activity and could tightly bind with the enzyme TK. Also, molecular docking analyses revealed that the structures of compounds and were suitable for TK inhibitory activity. Taken together, these results suggested that compounds and were promising herbicide candidates for weed control in wheat and maize fields targeting TK.
转酮醇酶（TK）是新型除草剂开发的潜在靶标。为了发现对抗性杂草有活性的新型 TK 抑制剂，设计并合成了 36 种含 1,2,4-三唑席夫碱的硫醚化合物，以评估其除草活性。结果表明，化合物 和 对测试杂草具有优异的除草效果，抑制率超过 90%，即使在 100mg/L 的低浓度下也是如此。此外，化合物 和 在温室中以 50-90g[有效成分（ai）]/ha 的剂量对测试杂草表现出比所有阳性对照更高的苗后除草活性，而在 90g（ai）/ha 的剂量下对玉米和小麦作物安全。荧光结合实验表明，化合物 和 对 TK 具有很强的抑制活性，能够与酶 TK 紧密结合。此外，分子对接分析表明，化合物 和 的结构适合 TK 抑制活性。综上所述，这些结果表明，化合物 和 是具有潜力的除草剂候选物，可用于防治小麦和玉米田中的 TK 靶标杂草。
