Xu F Z, Wang Y Y, Luo D X, Yu G, Guo S X, Fu H, Zhao Y H, Wu J
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 P. R. China
Institute for the Control of Agrochemicals, Ministry of Agriculture Beijing 100125 China.
RSC Adv. 2018 Feb 7;8(12):6306-6314. doi: 10.1039/c8ra00161h. eCollection 2018 Feb 6.
A series of trifluoromethyl pyridine derivatives containing 1,3,4-oxadiazole moiety was designed, synthesized and bio-assayed for their insecticidal activity. The result of bio-assays indicated the synthesized compounds exhibited good insecticidal activity against and , most of the title compounds show 100% insecticidal activity at 500 mg L and >80% activity at 250 mg L against the two pests. Compounds E18 and E27 showed LC values of 38.5 and 30.8 mg L against , respectively, which were close to that of avermectin (29.6 mg L); compounds E5, E6, E9, E10, E15, E25, E26, and E27 showed 100% activity at 250 mg L, which were better than chlorpyrifos (87%). CoMFA and CoMSIA models with good predictability were proposed, which revealed the electron-withdrawing groups with an appropriate bulk at 2- and 4-positions of benzene ring could enhance insecticidal activity.
设计、合成了一系列含有1,3,4-恶二唑部分的三氟甲基吡啶衍生物，并对其杀虫活性进行了生物测定。生物测定结果表明，合成的化合物对[具体害虫1]和[具体害虫2]表现出良好的杀虫活性，大多数目标化合物在500mg/L时表现出100%的杀虫活性，在250mg/L时对这两种害虫的活性>80%。化合物E18和E27对[具体害虫1]的LC值分别为38.5mg/L和30.8mg/L，接近阿维菌素的LC值（29.6mg/L）；化合物E5、E6、E9、E10、E15、E25、E26和E27在250mg/L时表现出100%的活性，优于毒死蜱（87%）。提出了具有良好预测性的CoMFA和CoMSIA模型，结果表明苯环2-位和4-位带有适当体积的吸电子基团可增强杀虫活性。
