Novel pyrazole carboxamides with a diarylamine-modified scaffold were modified based on the bixafen (Bayer) fungicide, which has excellent activity against Rhizoctonia solani, Rhizoctonia cerealis and Sclerotinia sclerotiorum. To discover the potential insecticidal activity of these novel pyrazole carboxamides, the present study explored their possible cytoactivity on the insect neuronal cells (RP-HzVNC-AW1) in Helicoverpa zea. The preliminary bioassays showed that some of the target compounds exhibited good cytoactivity against AW1 cells. Among them, compounds a5 and b4–b7 showed good activity in vitro with IC₅₀ values of 11.28, 10.46, 9.04, 11.72 and 12.19 μM, respectively. Notably, the IC₅₀ value of compound b5 was better than 11.81 μM for fipronil. We subsequently attempted to illustrate the mechanism of b5. Intracellular biochemical assays showed that b5 induced AW1 cell apoptosis with a decrease in themitochondrial membrane potential, as well as a significantly increased intracellular calcium ion concentration and caspase-3 activity. A significant decrease in Bcl-2 levels and a marked augmentation of cytochrome-c and Bax were also detected. These results indicate that a mitochondrially dependent intrinsic pathway contributes to compound b5-induced apoptosis in AW1 cells. This study suggests that b5 may act as a potential insecticide that can be used for further optimization.

具有联芳基胺改性支架的新型吡唑羧酰胺是基于联苯沙芬（Bayer）杀真菌剂进行修饰的，该联苯甲酰胺对solani solani，Rhizoctonia grainis和Sclerotiorum sclerotiorum具有优异的活性。为了发现这些新型吡唑羧酰胺的潜在杀虫活性，本研究探索了它们对Helicoverpa zea昆虫神经元细胞（RP-HzVNC-AW1）的可能的细胞活性。初步的生物测定表明，某些目标化合物对AW1细胞表现出良好的细胞活性。其中，化合物a5和b4 – b7在IC ₅₀体外显示出良好的活性分别为11.28、10.46、9.04、11.72和12.19μM。值得注意的是，化合物b5的氟虫腈的IC ₅₀值优于11.81μM。我们随后尝试说明b5的机制。细胞内生化分析表明，b5诱导AW1细胞凋亡，线粒体膜电位降低，细胞内钙离子浓度和caspase-3活性显着增加。还检测到Bcl-2水平显着下降以及细胞色素c和Bax明显增加。这些结果表明线粒体依赖性内在途径有助于化合物b5诱导的AW1细胞凋亡。这项研究表明b5可能充当潜在的杀虫剂，可用于进一步优化。