Phenylpyrazole insecticides are successful for crop protection and public hygiene by blocking gamma-aminobutyric acid (GABA)-gated chloride channels and glutamate-gated chloride (GluCl) channels. A series of novel phenylpyrazoles containing arylimine or 1-methoxyaryl groups were designed and synthesized. The addition reaction of methanol to the imines 1–11 was investigated and the cayno addition products 13–15 were obtained. The compounds 1–15 were confirmed by ¹H NMR and elemental analysis. The results of bioassay indicated that some compounds exhibited comparable bioactivity to fipronil against a broad spectrum of insects such as bean aphid (Aphis craccivora), mosquito (Culex pipiens pallens), diamondback moth (Plutella xylostella) and Oriental armyworm (Mythimna separata). Especially, the foliar contact activity against bean aphid of compound 7 at 10 µg mL⁻¹ was 68%, the larvacidal activity against mosquito of compounds 5, 13 and 15 at 0.0025 µg mL⁻¹ was 100%, the larvacidal activity against diamondback moth of compounds 9 and 11 at 0.05 µg mL⁻¹ was 100%, the larvacidal activity against Oriental armyworm of compound 9 at 1 µg mL⁻¹ was 100%. The 3-cayno moiety on pyrazole ring was essential for the high insecticidal activities against bean aphid, diamondback moth and Oriental armyworm, while the 3-carbimidate moiety on pyrazole ring was crucial to the excellent high insecticidal activities against mosquito.

苯并吡唑类杀虫剂通过阻断γ-氨基丁酸（GABA）门控的氯离子通道和谷氨酸门控氯化物（GluCl）通道，成功地实现了作物保护和公共卫生。设计并合成了一系列新的含有芳嘌呤或1-甲氧基芳基的苯基吡唑。甲醇的加成反应的亚胺1 - 11进行了研究和cayno加成产物13 - 15获得。化合物1 - 15经证实¹ H NMR和元素分析。生物测定的结果表明，某些化合物对氟虫腈对多种昆虫（如豆蚜）具有相当的生物活性。蚜虫（Aphis craccivora），蚊子（Culex pipiens pallens），小菜蛾（Plutella xylostella）和东方粘虫（Mythimna separata）。特别是，针对化合物的蚕豆蚜叶面接触活性7在10μg毫升^-1为68％，而化合物的蚊子的larvacidal活动5，13和15在0.0025微克毫升^-1为100％，对小菜蛾的活性larvacidal 0.05 µg mL ^-1下化合物9和11的化合物为100％，化合物9对东方粘虫的杀幼虫活性1μgmL ^-1时为100％。吡唑环上的3-cayno部分对于豆蚜，小菜蛾和东方粘虫的高杀虫活性至关重要，而吡唑环上的3-carbimidate部分对出色的高灭蚊活性至关重要。