State-Key Laboratory and Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071, PR China.
Bioorg Med Chem Lett. 2013 Jul 1;23(13):3723-7. doi: 10.1016/j.bmcl.2013.05.013. Epub 2013 May 16.
46 Novel nonsymmetrical aromatic disulfides containing [1,3,4]thiadiazole or [1,3,4]oxadiazole groups were synthesized and their biological activities were evaluated as inhibitors of acetohydroxyacid synthase (AHAS, EC 2.2.1.6). Besides their strong in vitro inhibition against plant AHAS, compounds 3e and 3f also display 80-100% post-emergence herbicidal activities in greenhouse bioassay at 1500g /ha dosage. The assay of exogenous branched-chain amino acids supplementation on rape root growth of 3e suggests that the herbicidal activity has relationship with AHAS inhibition.
合成了 46 种新型非对称芳香二硫化物，其中含有[1,3,4]噻二唑或[1,3,4]恶二唑基团，并评估了它们作为乙酰羟酸合酶（AHAS，EC 2.2.1.6）抑制剂的生物活性。除了对植物 AHAS 的强烈体外抑制作用外，化合物 3e 和 3f 在 1500g /ha 剂量的温室生物测定中也表现出 80-100%的苗后除草活性。对 3e 抑制油菜根生长的外源支链氨基酸补充的测定表明，除草活性与 AHAS 抑制有关。
