To develop the novel ryanodine receptors (RyRs) insecticides, encouraged by our previous research work, a series of novel N-phenylpyrazole derivatives containing a polysubstituted phenyl ring scaffold were designed and synthesized. The bioassays results indicated that some title compounds exhibited excellent insecticidal activity. For oriental armyworm (Mythimna separata), compounds 7f, 7g, 7i and 7o at 0.5 mg L^-1 displayed 100% larvicidal activity, and even at 0.1 mg L^-1, 7o was 30% larvicidal activity, comparable to chlorantraniliprole (30%) and better than cyantraniliprole (10%). Compounds 7f and 7o had the median lethal concentrations (LC₅₀) of 8.83×10^-2 and 7.12×10^-2 mg L^-1, respectively, close to chlorantraniliprole (6.79×10^-2 mg L^-1). Additionally, for diamondback moth (Plutella xylostella), the larvicidal activity of compounds 7f and 7i were 90% and 70% at 0.01 mg L^-1, respectively, better than chlorantraniliprole (50%) and cyantraniliprole (40%). More impressively, the LC₅₀ value of 7f was 4.2×10^-3 mg L^-1, slightly lower than that of chlorantraniliprole (5.0×10^-3 mg L^-1). The molecular docking between compound 7f and RyRs of diamondback moth validated our molecular designation. Furthermore, the calcium imaging experiment explored the influence of compound 7o on the calcium homeostasis in the central neurons of the third larvae of oriental armyworm. The results of this study indicated that 7o is a potent novel lead targeting at RyRs.

为了开发新型的ryanodine受体（RyRs）杀虫剂，在我们先前的研究工作的鼓励下，设计并合成了一系列含有多取代苯环骨架的新型N-苯基吡唑衍生物。生物测定结果表明，一些标题化合物表现出优异的杀虫活性。对于东方粘虫（Mythimna separata），化合物7f，7g，7i和7o在0.5 mg L ^-1时表现出100％的杀幼虫活性，即使在0.1 mg L ^-1时，7o也是30％的杀幼虫活性，与氯噻菌胺（30％ ），且优于cyantraniliprole（10％）。化合物7f和7o的中位致死浓度（LC ₅₀）分别为8.83×10 ^-2和7.12×10 ^-2 mg L ^-1，接近氯氰菊酯（6.79×10 ^-2 mg L ^-1）。另外，对于小菜蛾（Plutella xylostella），化合物7f和7i在0.01 mg L ^-1时的杀幼虫活性分别为氯虫腈（50％）和氰基氰虫酯（40％）。更令人印象深刻的是，7f的LC ₅₀值为4.2×10 ^-3 mg L ^-1，比氯蒽醌的含量略低（5.0×10 ^-3 mg L ^-1）。小菜蛾的化合物7f和RyRs之间的分子对接验证了我们的分子命名。此外，钙成像实验探索了化合物7o对东方粘虫第三幼虫中枢神经元中钙稳态的影响。这项研究的结果表明7o是针对RyRs的有效新型铅。