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

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

  • J Agric Food Chem. 2024 Sep 4;72(35):19274-19285. doi: 10.1021/acs.jafc.4c01484.
Simin Wang 1 Zhixiang Zhao 1 Yiyang Wang 1 Haoyu Zheng 1 Qinyu Zhang 1 Li Zhang 1 Jianjun Zhang 1 Huizhe Lu 1 Yanhong Dong 1
Affiliations

Affiliation

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

Keywords

1,2,3-triazole; ergosterol; fungicidal activity; malononitrile; transcriptome analysis.

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