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Fungicidal Activity of Carboxamides Containing Spiropiperidinyl-α-methylene-γ-butyrolactones Targeting Oxysterol Binding Protein

文献类型： 外文期刊

作者： Yuan, Haolin 1 ; Wu, Rongzhang 1 ; Hu, Yangxiaochun 3 ; Zhang, Jin 1 ; Zhang, Yue 1 ; Wang, Zhihong 1 ; Huo, Jianfei 4 ; Tang, Liangfu 1 ; Zhao, Bin 5 ; Fan, Zhijin 1 ;

作者机构： 1.Nankai Univ, Coll Chem, State Key Lab Elemento Organ Chem, Tianjin 300071, Peoples R China

2.Nankai Univ, Coll Chem, Frontiers Sci Ctr New Organ Matter, Tianjin 300071, Peoples R China

3.China Agr Univ, Coll Sci, Beijing 100193, Peoples R China

4.Tianjin Acad Agr Sci, Inst Plant Protect, Tianjin 300384, Peoples R China

5.Hebei Agr Univ, Coll Plant Protect, State Key Lab North China Crop Improvement & Regul, Baoding 071001, Peoples R China

关键词： oxysterol binding protein; molecular design; fungicide

期刊名称：JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY （ 影响因子：6.2； 五年影响因子：6.4 ）

ISSN： 0021-8561

年卷期： 2025 年 73 卷 15 期

页码：

收录情况： SCI

摘要： Oxysterol binding protein (OSBP) is a new target for oomycide development. To find more fungicidal active compounds targeting OSBP, a series of carboxamides containing spiropiperidinyl-alpha-methylene-gamma-butyrolactone and heterocyclic carboxylic acids were rationally designed and synthesized by using a computer-aided pesticide design method. The in vitro fungicidal bioassay found that compound 5o showed broad-spectrum activity with EC50 values falling between 0.50 and 20.85 mu g/mL against Phytophthora capsici and Fusarium verticillioides, respectively, which was more potent than 7c and natural lead xanthatin. Compound 5o also showed 44% in vivo efficacy against Pseudoperonospora cubensis, even at a concentration of 0.5 mu g/mL. Fluorescence quenching and microscale thermophoresis determination suggested that compound 5o bound to Osh4p and showed stronger interactions than oxathiapiprolin. RNA sequencing analysis discovered that the ergosterol (ERG) gene cluster and ribosome biogenesis in eukaryotes were downregulated. Compound 5o was discovered as a good fungicidal candidate targeting OSBP deserving further studies.

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