Inspired by the wide application of amides in plant pathogens, a series of novel 1-substituted-5-trifluoromethyl‑1H‑pyrazole-4-carboxamide derivatives were designed and synthesized. Bioassay results indicated that some target compounds exhibited excellent and broad-spectrum in vitro and certain in vivo antifungal activities. Among them, the in vitro EC₅₀ values of Y₁₃ against G. zeae, B. dothidea, F. prolifeatum and F. oxysporum were 13.1, 14.4, 13.3 and 21.4 mg/L, respectively. The in vivo protective activity of Y₁₃ against G. zeae at 100 mg/L was 50.65%. SAR analysis revealed that the phenyl on the 1-position of the pyrazole ring was important for this activity. An antifungal mechanism study of Y₁₃ against G. zeae demonstrated that this compound may disrupt the cell membrane of mycelium, thus inhibiting the growth of fungi. These mechanistic study results were inconsistent with those for traditional amides and may provide a novel view for deep study of this series of pyrazole carboxamide derivatives.

受酰胺类在植物病原体中的广泛应用的启发，设计合成了一系列新型 1-取代-5-三氟甲基-1 H-吡唑-4-甲酰胺衍生物。生物测定结果表明，一些目标化合物在体外表现出优异的广谱性和一定的体内抗真菌活性。其中，Y ₁₃对玉米芽孢杆菌、多蒂芽孢杆菌、增殖镰刀菌和尖孢镰刀菌的体外EC ₅₀值分别为13.1、14.4、13.3和21.4mg /L。Y ₁₃的体内保护活性100 mg/L 的玉米杆菌为 50.65% 。SAR 分析表明，吡唑环 1 位上的苯基对该活性很重要。Y ₁₃对G. zeae的抗真菌机制研究表明，该化合物可能会破坏菌丝体的细胞膜，从而抑制真菌的生长。这些机理研究结果与传统酰胺的研究结果不一致，可能为深入研究该系列吡唑甲酰胺衍生物提供新的视角。