Background: Oxadiazole fragment is one of the most prevalent structures in biochemicals, especially in the research of new pesticides. It is necessary to develop new insecticides with a different mode of action for the treatment of insecticide resistance problems. And, it is worth exploring the new active insecticidal lead structures with oxadiazole fragments.

Methods: We used a “splicing up” method introducing the trifluoromethyl-oxadiazole moiety to 3- (ethylsulfonyl)-pyridine structure, and replaced the 6-position on the pyridine ring by different substituted amines. Then, a series of novel 3-(ethylsulfonyl)-pyridines containing trifluoromethyloxadiazole moiety were designed and synthesized. All these title compounds were confirmed by ¹H NMR, ¹³C NMR and ESI-MS.

Results: The primary insecticidal activity results indicated that some of them (A1-A7, A10, A13- A14) exhibited good mortality against Mythimna separate at 500 mg/L (80-100%), and compounds A13 and A14 have moderate insecticidal activity against M. separate at 250 mg/L (50-55%).

Discussion: The bioassay results showed that the designed compounds did not achieve excellent insecticidal activity by introducing the potential oxadiazole fragment. Therefore, it seems that the special physicochemical properties of the oxadiazole fragment should be considered in fragment splicing-based design.

Conclusion: According to the bioassay studies, the results revealed that compounds A13 and A14 may provide useful information for further designing of efficient insecticides.

背景：恶二唑片段是生物化学中最流行的结构之一，尤其是在新农药的研究中。有必要开发具有不同作用方式的新型杀虫剂来治疗杀虫剂抗性问题。并且，值得探索具有恶二唑片段的新型活性杀虫铅结构。

方法：我们采用“拆分”方法，将三氟甲基-恶二唑部分引入到3-（乙基磺酰基）-吡啶结构中，并用不同的取代胺取代了吡啶环上的6位。然后，设计并合成了一系列新颖的含有三氟甲基恶二唑部分的3-（乙基磺酰基）-吡啶。所有这些标题化合物通过¹ H NMR，¹³ C NMR和ESI-MS证实。

结果：初步杀虫活性结果表明，其中一些（A1-A7，A10，A13-A14）分别以500 mg / L（80-100％）表现出对Mythimna的良好杀灭作用，化合物A13和A14具有中等杀虫活性。相对于M.的分离浓度为250 mg / L（50-55％）。

讨论：生物测定结果表明，通过引入潜在的恶二唑片段，所设计的化合物没有实现出色的杀虫活性。因此，似乎在基于片段剪接的设计中应考虑恶二唑片段的特殊理化性质。

结论：根据生物测定研究，结果表明化合物A13和A14可能为进一步设计有效的杀虫剂提供有用的信息。