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新型含 1,2,3-三唑的丙二腈衍生物的设计、合成与生物活性测定。

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

机构信息

Department of Applied Chemistry, College of Science, China Agricultural University, Beijing 100193, China.

出版信息

J Agric Food Chem. 2024 Sep 4;72(35):19274-19285. doi: 10.1021/acs.jafc.4c01484. Epub 2024 Aug 26.

DOI:10.1021/acs.jafc.4c01484
PMID:39185617
Abstract

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 () containing 1,2,3-triazole and malononitrile structures were synthesized. When the compounds were tested against six fungal species, they exhibited significant fungicidal activity toward and . Compounds and displayed promising efficacy, with an EC of 0.19 and 0.27 mg/L respectively against . Fungal ergosterol production was suppressed by compounds and , according to a preliminary analysis of their mechanism of action on using transcriptomics and scanning electron microscopy. It has been shown through experimentation that compounds and prevent from synthesizing ergosterol. Ultimately, it was anticipated that compounds and would be discovered to be low-toxic.

摘要

使用抗真菌农用化学品作为最经济的解决方案可能会减少由病原真菌引起的植物病害,这些病害对全球粮食的质量和产量有重大的负面影响。在这项工作中,合成了 33 种含有 1,2,3-三唑和丙二腈结构的化合物()。当测试这些化合物对六种真菌物种时,它们对 和 表现出显著的杀菌活性。化合物 和 表现出有希望的防治效果,对 的 EC 分别为 0.19 和 0.27mg/L。根据对 用转录组学和扫描电子显微镜进行的作用机制的初步分析,化合物 和 抑制了真菌麦角甾醇的产生。通过实验表明,化合物 和 阻止 合成麦角甾醇。最终,预计会发现化合物 和 是低毒的。

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