曾令强, 罗睿童, 陈琼, 郝格非, 朱晓磊, 杨光富. 杀菌剂氟苯醚酰胺的创制[J]. 农药学学报, 2022, 24(5): 895-903. DOI: 10.16801/j.issn.1008-7303.2022.0028
    引用本文: 曾令强, 罗睿童, 陈琼, 郝格非, 朱晓磊, 杨光富. 杀菌剂氟苯醚酰胺的创制[J]. 农药学学报, 2022, 24(5): 895-903. DOI: 10.16801/j.issn.1008-7303.2022.0028
    ZENG Lingqiang, LUO Ruitong, CHEN Qiong, HAO Gefei, ZHU Xiaolei, YANG Guangfu. Discovery of fungicide flubeneteram[J]. Chinese Journal of Pesticide Science, 2022, 24(5): 895-903. DOI: 10.16801/j.issn.1008-7303.2022.0028
    Citation: ZENG Lingqiang, LUO Ruitong, CHEN Qiong, HAO Gefei, ZHU Xiaolei, YANG Guangfu. Discovery of fungicide flubeneteram[J]. Chinese Journal of Pesticide Science, 2022, 24(5): 895-903. DOI: 10.16801/j.issn.1008-7303.2022.0028

    杀菌剂氟苯醚酰胺的创制

    Discovery of fungicide flubeneteram

    • 摘要: 琥珀酸脱氢酶 (succinate dehydrogenase, SDH) 是重要的杀菌剂靶标之一,而很多植物病原菌对靶向SDH的杀菌剂已经产生了较为严重的抗药性,因此新型靶向SDH的杀菌剂设计显得尤为重要。基于药效团连接碎片的虚拟筛选 (PFVS) 是一种独立于生物物理技术的高通量药物发现方法,采用PFVS方法成功获得了靶向SDH的新型杀菌剂候选化合物—氟苯醚酰胺。本文主要从PFVS原理、先导化合物的发现、取代基的修饰以及杀菌活性研究等方面对氟苯醚酰胺的创制进行系统分析。氟苯醚酰胺创制的案例分析可为农药研究工作者提供新思路和新方法。

       

      Abstract: Succinate dehydrogenase (SDH) is one of the important fungicide targets. However, many plant pathogens showed medium and even high resistance to commercial fungicides targeting upon SDH. So, it is very urgent to design new novel inhibitor for SDH. Pharmacophore-linked fragment virtual screening (PFVS) is a high-throughput drug discovery approach independent of biophysical screening techniques and flubeneteram, a novel fungicide candidate targeting SDH, was successfully obtained by PFVS. Here, the development process of the fungicide flubeneteram was analyzed in detail, including the principle of PFVS, the discovery of lead compounds, the modification of substituents and the fungicidal activity. The discovery process of flubeneteram would provide novel ideas and methods for pesticide researchers.

       

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