新型噻唑烷酮三氟乙基亚砜类化合物的设计、合成及杀螨活性

    Design, synthesis and acaricidal activity of novel thiazolidinone containing trifluoroethyl sulfoxide compounds

    • 摘要: 为寻找高杀螨活性化合物,以团队前期报道的螺噻唑烷酮三氟乙基硫醚化合物为先导,设计并合成了25个新型噻唑烷酮三氟乙基亚砜类衍生物。所有化合物结构均经核磁共振氢谱(1H NMR)、碳谱(13C NMR)和高分辨质谱(HRMS)确证。生测结果显示:100 mg/L下,部分化合物对朱砂叶螨(Tetranychus cinnabarinus)和二斑叶螨(T. urticae)的致死率大于90%;其中,化合物Ⅲe对朱砂叶螨的半数致死浓度(LC50)低至3.8 mg/L,活性优于先导化合物(4.3 mg/L),可作为新一代高活性杀螨剂候选化合物进行深度研究与开发。

       

      Abstract: To discover new acaricides with high activities, 25 novel thiazolidinones containing trifluoroethyl sulfoxide compounds were designed and synthesized based on the lead compound—spirothiazolidinones containing trifluoroethyl sulfide moiety, which was reported in our previous work. All the designed compounds were characterized by 1H NMR, 13C NMR and HRMS. Acaricidal activity tests showed that some of the designed compounds exhibited more than 90% activity against Tetranychus cinnabarinus and T. urticae at a dosage of 100 mg/L. Notably, compound Ⅲe was effective against T. cinnabarinus with the lethal concentration 50 (LC50) value of 3.8 mg/L, which exhibited higher activity than the lead compound (4.3 mg/L). This compound can serve as a promising candidate for further development as a new generation of high-efficacy acaricid.

       

    /

    返回文章
    返回