Design, Synthesis, and Biological Activities of Novel 1,3,5-Trimethylpyrazole-Containing Malonamide Derivatives

文献类型： 外文期刊

第一作者： Liao, Min

作者： Liao, Min;Liu, Qing;Feng, Tong;Xu, Zhi-Yuan;Liu, Shang-Zhong;Rui, Chang-Hui

作者机构：

关键词： malonamide; pyflubumide; synthesis; acaricidal and insecticidal activities

期刊名称：MOLECULES （ 影响因子：4.411； 五年影响因子：4.587 ）

ISSN： 1420-3049

年卷期： 2019 年 24 卷 3 期

页码：

收录情况： SCI

摘要： New 1,3,5-trimethylpyrazole-containing malonamide derivatives based on pyflubumide were designed, synthesized, and characterized using H-1-NMR, C-13-NMR, and high-resolution mass spectra (HRMS). The results of preliminary bioassays showed that the target compounds possessed good activities against Tetranychus cinnabarinus, Plutella xylostella, and Aphis craccivora. Most of the target compounds exhibited moderate to good acaricidal activity against Tetranychus cinnabarinus at a concentration of 400 mu g/mL, and some showed moderate activity at a concentration of 200 mu g/mL; in particular, compounds 8m and 8p exhibited 70.0% mortality. In addition, some of the target compounds exhibited good insecticidal activities against Plutella xylostella at a concentration of 200 mu g/mL, especially compounds 8i and 8o, which achieved 100.0% mortality at a concentration of 100 mu g/mL. Interestingly, some of the target compounds exhibited potent anti-aphid activity against Aphis craccivora at a concentration of 200 mu g/mL; furthermore, compounds 8p and 8q demonstrated 100.0% anti-aphid activity at a concentration of 50 mu g/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.

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