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Novel amide derivatives containing a pyridine moiety: design, synthesis as potential fungicides

文献类型： 外文期刊

作者： Luo, Xin 1 ; Chen, Yifang 1 ; Wang, Yu 1 ; Xing, Zhifu 1 ; Peng, Ju 1 ; Yi, Chongfen 2 ; Chen, Jixiang 1 ;

作者机构： 1.Guizhou Univ, Ctr R&D Fine Chem, Natl Key Lab Green Pesticide, Key Lab Green Pesticide & Agr Bioengn,Minist Educ, Guiyang 550025, Peoples R China

2.Guizhou Acad Agr Sci, Guizhou Rice Res Inst, Guiyang, Peoples R China

关键词： Amide derivatives; Antifungal activity; Molecular docking; Succinate dehydrogenase inhibitors; Mycelial morphology; RT-qPCR

期刊名称：CHEMICAL PAPERS （ 影响因子：2.2； 五年影响因子：2.0 ）

ISSN： 0366-6352

年卷期： 2023 年

页码：

收录情况： SCI

摘要： To discover new fungicides, a series of amides derivatives containing a pyridine moiety were designed and synthesized by grafting the pyridine of fluopyram into the boscalid structure. The EC50 values of compounds 9, 11, and 15 against Rhizoctonia solani (R. solani) were 0.19, 0.83, and 0.09 mg/L, respectively, which were better than the control agent boscalid (1.70 mg/L). The EC50 values of compounds 15 against Monilinia fructicola (M. fructicola) were 5.46 mg/L. The protective activity of compound 15 against rice sheath blight was 74.1% at 100 mg/L, which was better than boscalid (54.6%). In addition, the inhibition of SDH by compound 15 was 0.11 & mu;mol/L, which was better than that of boscalid (8.22 & mu;mol/L). The molecular docking results were consistent with the antifungal activity and SDH inhibitory activity. Interestingly, compound 15 can significantly reduce the expression level of SDHB and SDHD. Compound 15 can be used as a lead structure to develop SDH inhibitors.

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