Novel quinoxalinone-1,2,3-triazole derivatives as potential antifungal agents for plant anthrax disease: Design, synthesis, antifungal activity and SAR study

Advanced Agrochem Pub Date : 2023-11-25 DOI:10.1016/j.aac.2023.11.003

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Abstract

A series of quinoxalinone-1,2,3-triazole derivatives have been synthesized and tested for antifungal activity against phytopathogenic fungus through mycelial growth inhibition in vitro, spore germination inhibition in vitro and control effect in vivo. The results showed that the pharmacophore quinoxalinone and 1,2,3-triazole displayed promising antifungal activity. The EC50 value against C. gloeosporioides of 6a-1 was 1.17 μg/mL and the compound 6c-1 showed the good bioactivity against C. fragariae Brooks and P. oryzae Cav., displaying EC50 values of 5.56, 4.62 μg/mL, respectively. The inhibitory of spore germination by 6a-1 was performed with EC50 value of 1.91 μg/mL. In addition, the in vivo bioassay indicated that 6a-1 possessed effective control against Pepper Anthrax Disease in protective treatment. For given activity data of target compounds, structure-activity relationship (SAR) study was operated, hoping for optimizing the target structure to find lead compound with higher activity.

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新型喹喔啉酮-1,2,3-三唑衍生物作为植物炭疽病的潜在抗真菌剂：设计、合成、抗真菌活性和 SAR 研究

本研究合成了一系列喹喔啉酮-1,2,3-三唑衍生物，并通过体外菌丝生长抑制、体外孢子萌发抑制和体内对照效应测试了这些衍生物对植物病原真菌的抗真菌活性。结果表明，药源喹喔啉酮和 1,2,3- 三唑具有良好的抗真菌活性。化合物 6c-1 对 C. fragariae Brooks 和 P. oryzae Cav.具有良好的生物活性，其 EC50 值分别为 5.56 和 4.62 μg/mL。6a-1 对孢子萌发的抑制作用的 EC50 值为 1.91 μg/mL。此外，体内生物测定表明，6a-1 在保护性治疗中可有效控制辣椒炭疽病。针对目标化合物的活性数据，研究人员进行了结构-活性关系（SAR）研究，希望通过优化目标化合物的结构，找到活性更高的先导化合物。

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来源期刊

Advanced Agrochem

CiteScore

3.50

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0.00%

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