In this study, 24 indole derivatives containing 1,3,4-thiadiazole were discovered and synthesized. The target compounds’ antifungal efficacy against 14 plant pathogenic fungal pathogens was then determined in vitro. With an EC₅₀ value of 2.7 μg/mL, Z2 demonstrated the highest level of bioactivity among them against Botrytis cinerea (B.c.), exceeding the concentrations of the control prescription drugs azoxystrobin (Az) (EC₅₀ = 14.5 μg/mL) and fluopyram (Fl) (EC₅₀ = 10.1 μg/mL). Z2 underwent in vivo testing on blueberry leaves in order to evaluate its usefulness in real-world settings. A reasonable protective effect was obtained with a control effectiveness of 93.0% at 200 μg/mL, which was superior to those of Az (83.0%) and Fl (52.0%). At 200 μg/mL, this chemical had an efficacy of 84.0% in terms of curative efficacy. These figures outperformed those of Az (69.0%) and Fl (48.0%). Scanning electron microscopy (SEM) experiments and light microscopy experiments showed that Z2 altered the integrity of the cell wall and cell membrane of the pathogenic fungus B.c., which led to an increase in the content of malondialdehyde (MDA), cellular leakage, and cellular permeability. Enzyme activity assays and molecular docking studies indicated that Z2 could act as a potential succinate dehydrogenase inhibitor (SDHI). It was hypothesized that Z2 could cause disruption of mycelial cell membranes, which in turn leads to mycelial death. According to the research, indole derivatives containing 1,3,4-thiadiazole were expected to evolve into new fungicides due to their significant antifungal effects on plant fungi.

中文翻译：

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含1,3,4-噻二唑的新型吲哚衍生物的抗真菌活性

本研究发现并合成了24种含有1,3,4-噻二唑的吲哚衍生物。然后在体外测定了目标化合物对 14 种植物病原真菌病原体的抗真菌功效。Z2的 EC ₅₀值为 2.7 μg/mL，显示出其中针对灰葡萄孢( Bc .) 的最高水平的生物活性，超过了对照处方药嘧菌酯 (Az) 的浓度 (EC ₅₀ = 14.5 μg/mL) 和氟吡菌酰胺 (Fl) (EC ₅₀ = 10.1 μg/mL)。Z2在蓝莓叶上进行了体内测试，以评估其在现实环境中的有用性。 200 μg/mL浓度下，防效达93.0%，优于Az（83.0%）和Fl（52.0%）。在200μg/mL时，该化学品的疗效为84.0%。这些数字优于 Az (69.0%) 和 Fl (48.0%)。扫描电镜（SEM）实验和光镜实验表明，Z2改变了病原真菌Bc .细胞壁和细胞膜的完整性，导致丙二醛（MDA）含量增加，细胞渗漏，细胞渗透性。酶活性测定和分子对接研究表明，Z2可以作为潜在的琥珀酸脱氢酶抑制剂 (SDHI)。据推测，Z2可能会导致菌丝体细胞膜破裂，进而导致菌丝体死亡。研究表明，含有1,3,4-噻二唑的吲哚衍生物由于对植物真菌具有显着的抗真菌作用，有望演变成新型杀菌剂。