State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Research and Development Center for Fine Chemicals , Guizhou University , Huaxi District, Guiyang 550025 , China.
J Agric Food Chem. 2018 Sep 19;66(37):9616-9623. doi: 10.1021/acs.jafc.8b03020. Epub 2018 Sep 10.
A series of novel 1,3,4-oxadiazole-cinnamic acid hybrids were synthesized. The bioassays results indicated that compounds 1, 2, 7, and 8 showed excellent nematicidal activities against Tylenchulus semipenetrans with LC values of 9.7 ± 1.6, 15.6 ± 2.8, 8.0 ± 0.5, and 19.8 ± 2.9 mg/L, respectively, which were higher than those of avermectin (32.6 ± 4.5 mg/L) and fosthiazate (67.8 ± 1.7 mg/L). Low-toxicity compound 26, with excellent nematicidal activity in vitro (LC = 8.2 ± 1.2 mg/L), was designed on the basis of the predictive CoMFA ( q = 0.795, r = 0.921) and CoMSIA ( q = 0.762, r = 0.912) models. The control effect of compound 26 was 69.8% at an effective dose of 1.0 g per plant in a field experiment, which was superior to that of fosthiazate (67.2%). This work indicated that 1,3,4-oxadiazole-cinnamic acid hybrids may be used as potential nematicides.
一系列新型 1,3,4-噁二唑-肉桂酸杂合体被合成。生物测定结果表明，化合物 1、2、7 和 8 对茶藨根结线虫具有优异的杀线虫活性，LC 值分别为 9.7 ± 1.6、15.6 ± 2.8、8.0 ± 0.5 和 19.8 ± 2.9 mg/L，高于阿维菌素（32.6 ± 4.5 mg/L）和噻唑膦（67.8 ± 1.7 mg/L）。低毒性化合物 26，体外杀线虫活性优异（LC = 8.2 ± 1.2 mg/L），是基于预测 CoMFA（q = 0.795，r = 0.921）和 CoMSIA（q = 0.762，r = 0.912）模型设计的。在田间试验中，化合物 26 在有效剂量为 1.0 g/株时的防治效果为 69.8%，优于噻唑膦（67.2%）。这项工作表明，1,3,4-噁二唑-肉桂酸杂合体可能被用作有潜力的杀线虫剂。
