Design, Synthesis, and Bioactivity Determination of Novel Malononitrile Derivatives Containing 1,2,3-Triazole

丙二腈 1,2,4-三唑 组合化学 三唑 化学 有机化学 催化作用
作者
Simin Wang,Zhixiang Zhao,Yiyang Wang,Haoyu Zheng,Qinyu Zhang,Li Zhang,Jianjun Zhang,Huizhe Lu,Yanhong Dong
出处
期刊:Journal of Agricultural and Food Chemistry [American Chemical Society]
卷期号:72 (35): 19274-19285 被引量:11
标识
DOI:10.1021/acs.jafc.4c01484
摘要

Using antifungal agrochemicals as the most economical solution might reduce plant diseases caused by pathogenic fungi, which have a significant negative impact on the quality and yield of food worldwide. In this work, 33 compounds (G) containing 1,2,3-triazole and malononitrile structures were synthesized. When the compounds were tested in vitro against six fungal species, they exhibited significant fungicidal activity toward Botrytis cinerea and Rhizoctonia solani. Compounds G17 and G30 displayed promising in vivo efficacy, with an EC50 of 0.19 and 0.27 mg/L respectively against R. solani. Fungal ergosterol production was suppressed by compounds G17 and G30, according to a preliminary analysis of their mechanism of action on R. solani using transcriptomics and scanning electron microscopy. It has been shown through experimentation that compounds G17 and G30 prevent R. solani from synthesizing ergosterol. Ultimately, it was anticipated that compounds G17 and G30 would be discovered to be low-toxic.
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