A series of flavonoid derivatives containing 1,2,4-triazolo[4,3-]pyridine were designed, synthesized and evaluated for their antifungal activity. Bioactivity tests showed that some target compounds exhibited the strong antifungal activity against (), (), and . Among them, the half maximal effective concentration (EC) value of against was 3.3 μg/mL, which was less than that of the control drug azoxystrobin (21.0 μg/mL). The EC value of against was 12.7 μg/mL, which was better than that of azoxystrobin (28.1 μg/mL). In addition, the protective and curative activities of against blueberry were 92.0 and 79.8 % at 200 μg/mL, respectively, which were higher than those of the control drug azoxystrobin (89.4 and 71.7 %). Scanning electron microscopy (SEM) and spore germination experiments showed that could not only cause the mycelium damage but also inhibited the spore germination. Fluorescence microscopy (FM) observation, relative electrical conductivity measurement and cytoplasmic leakage assays indicated that could affect cell membrane integrity by inducing lipid peroxidation and increasing cell membrane permeability as well as causing leakage of cytoplasmic contents. These results show that flavonoid derivatives containing 1,2,4-triazolo[4,3-]pyridine had excellent inhibitory effects on , providing another supplement for the development of new pesticides.

中文翻译：

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含有 1,2,4-三唑并[4,3-a]吡啶的新型黄酮衍生物作为潜在抗真菌剂：设计、合成和生物学评价

设计、合成了一系列含有1,2,4-三唑并[4,3-]吡啶的黄酮类衍生物并评价其抗真菌活性。生物活性测试表明，部分目标化合物对()、()和 表现出较强的抗真菌活性。其中，抗的半数最大有效浓度（EC）值为3.3 μg/mL，低于对照药嘧菌酯（21.0 μg/mL）。抗的EC值为12.7 μg/mL，优于嘧菌酯(28.1 μg/mL)。此外，在200 μg/mL浓度下，对蓝莓的保护活性和治疗活性分别为92.0%和79.8%，高于对照药物嘧菌酯（89.4%和71.7%）。扫描电镜(SEM)和孢子萌发实验表明，不仅会造成菌丝体损伤，而且会抑制孢子萌发。荧光显微镜（FM）观察、相对电导率测量和细胞质渗漏测定表明，它可以通过诱导脂质过氧化、增加细胞膜通透性以及导致细胞质内容物渗漏来影响细胞膜完整性。这些结果表明，含有1,2,4-三唑并[4,3-]吡啶的黄酮类衍生物具有优异的抑制作用，为新型农药的开发提供了又一补充。