Design, Synthesis and Insecticidal Activity of Novel meta-Diamide Compounds Containing Pyridine Rings,Chemistry & Biodiversity

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Design, Synthesis and Insecticidal Activity of Novel meta-Diamide Compounds Containing Pyridine Rings
Chemistry & Biodiversity ( IF 2.3 ) Pub Date : 2024-04-27 , DOI: 10.1002/cbdv.202400816
Yanyu Yao ₁ , Jiyong Liu ₂ , Liqi Zhou ₂ , Tingting Zhao ₂ , Zhen He ₁ , Hang Gong _{1,

3} , Kangming Li ₂

Affiliation

In order to discover new meta-diamide compounds with good activity and novel structure, 15 related compounds were designed and synthesized by the bioisosterism principle with cyproflanilide as the lead compound. The insecticidal activities of these compounds against Plutella xylostella and Tetranychus cinnabarinus were tested, and the results of biological activity test showed that some compounds had more than 90 % insecticidal activity against Plutella xylostella at 1 mg/L and Tetranychus cinnabarinus at 100 mg/L. Especially, N-(2-bromo-6-(difluoromethoxy)-4-(perfluoro propan-2-yl)phenyl)-6-(isonicotinamido)picolinamide against Tetranychus cinnabarinus at 10 mg/L was 100 %, which was better than that of cyproflanilide. Molecular docking studies suggested that N-(2-bromo-6-(difluoromethoxy)-4-(perfluoropropan-2-yl)phenyl)-6-(4-cyano-2-methylbenzamido)picolinamide had a closely combined with the Plutella xylostella 3RHW (a glutamate-gated chloride channel). This study provides an avenue for designing and synthesizing a new generation of more effective pesticides.

中文翻译：

新型含吡啶环间二酰胺化合物的设计、合成及杀虫活性

为了发现活性良好、结构新颖的新型间二酰胺化合物，以环丙苯胺为先导化合物，利用生物电子等排原理设计合成了15个相关化合物。测试了这些化合物对小菜蛾和朱砂叶螨的杀虫活性，生物活性测试结果表明，部分化合物对1 mg/L的小菜蛾和100 mg/L的朱砂叶螨具有90%以上的杀虫活性。其中， N- (2-溴-6-(二氟甲氧基)-4-(全氟丙-2-基)苯基)-6-(异烟酰胺)吡啶酰胺在10mg/L时对朱砂叶螨的杀灭效果为100%，优于环丙苯胺。分子对接研究表明N- (2-bromo-6-(二氟甲氧基)-4-(全氟丙-2-基)苯基)-6-(4-氰基-2-甲基苯甲酰胺基)吡啶酰胺与小菜蛾紧密结合。 3RHW（谷氨酸门控氯离子通道）。这项研究为设计和合成新一代更有效的农药提供了途径。

更新日期：2024-04-27

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