Department of Applied Chemistry, College of Science, China Agricultural University, Beijing 100193, China.
Key Laboratory of Integrated Pest Management in Crops, Ministry of Agriculture, Institute of Plant Protection, Chinese Academy of Agricultural Sciences, Beijing 100193, China.
Molecules. 2019 Feb 3;24(3):562. doi: 10.3390/molecules24030562.
New 1,3,5-trimethylpyrazole-containing malonamide derivatives based on pyflubumide were designed, synthesized, and characterized using ¹H-NMR, C-NMR, and high-resolution mass spectra (HRMS). The results of preliminary bioassays showed that the target compounds possessed good activities against , , and . Most of the target compounds exhibited moderate to good acaricidal activity against at a concentration of 400 µg/mL, and some showed moderate activity at a concentration of 200 µg/mL; in particular, compounds and exhibited 70.0% mortality. In addition, some of the target compounds exhibited good insecticidal activities against at a concentration of 200 µg/mL, especially compounds and which achieved 100.0% mortality at a concentration of 100 µg/mL. Interestingly, some of the target compounds exhibited potent anti-aphid activity against at a concentration of 200 µg/mL; furthermore, compounds and demonstrated 100.0% anti-aphid activity at a concentration of 50 µg/mL. The preliminary analyses of the structure⁻activity relationships (SAR) indicated that the acaricidal and insecticidal activities varied significantly depending on the type of substituent and substitution pattern, which provides guidance for the further investigation of such structural modifications.
基于吡氟草胺，设计、合成并通过 ¹H-NMR、C-NMR 和高分辨率质谱（HRMS）对新的 1,3,5-三甲基吡唑基丙二酰胺衍生物进行了表征。初步生物测定结果表明，目标化合物对 、 、 具有良好的活性。大多数目标化合物在 400µg/mL 浓度下对 具有中等至良好的杀螨活性，一些化合物在 200µg/mL 浓度下表现出中等活性；特别是化合物 和 表现出 70.0%的死亡率。此外，一些目标化合物在 200µg/mL 浓度下对 表现出良好的杀虫活性，特别是化合物 和 在 100µg/mL 浓度下达到 100.0%的死亡率。有趣的是，一些目标化合物在 200µg/mL 浓度下对 表现出很强的抗蚜活性；此外，化合物 和 在 50µg/mL 浓度下表现出 100.0%的抗蚜活性。结构-活性关系（SAR）的初步分析表明，杀螨和杀虫活性随取代基的类型和取代模式有显著变化，为进一步进行此类结构修饰提供了指导。
