您好，欢迎访问湖北省农业科学院 机构知识库！
湖北省农业科学院机构知识库

全部

  • 全部
  • 标题
  • 学者
  • 机构
  • 关键词

Synthesis and Evaluation of Antifungal Activity of Novel Potent SDHI Fungicides Featuring a Conjugated Alkyne Structural Motif

文献类型： 外文期刊

作者： Bao, Longzhu 1 ; Zhou, Zifei 1 ; Chen, Yu 3 ; Yan, Xiaolong 1 ; Xu, Weilong 1 ; Li, Jun 1 ; Zhai, Qianqian 1 ; Ke, Shaoyong 2 ; Teng, Huailong 1 ;

作者机构： 1.Huazhong Agr Univ, Coll Chem, Wuhan 430070, Hubei, Peoples R China

2.Hubei Acad Agr Sci, Natl Biopesticide Engn Res Ctr, Hubei Biopesticide Engn Res Ctr, Key Lab Microbial Pesticides,Minist Agr & Rural Af, Wuhan 430064, Peoples R China

3.Univ Nottingham Ningbo China, Fac Off Sci & Engn, Dept Chem & Environm Engn, Ningbo 315100, Peoples R China

关键词： conjugated alkyne; succinate dehydrogenase; fungicides; enzyme activity; molecular docking

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 24 期

页码：

收录情况： SCI

摘要： The productivity and quality of agricultural commodities are significantly affected by plant pathogenic fungi, thereby necessitating the urgent development of new fungicides with specific structures, high efficacy, and low toxicity. In this study, a series of novel conjugated alkynes as succinate dehydrogenase inhibitors were synthesized, and their antifungal properties were evaluated. The bioassay results demonstrated that most synthesized compounds exhibited greater potency against Rhizoctonia solani than other fungal species. Specifically, compounds 4 and 16 exhibited remarkable in vitro inhibitory effects against Rhizoctonia solani, with EC50 values of 0.05 and 0.20 mu mol/L, respectively. This signifies a noteworthy enhancement compared to the control Boscalid, which exhibited an EC50 value of 1.55 mu mol/L. Moreover, compound 16 demonstrated a relatively broad-spectrum antifungal activity against five additional pathogenic fungi and exhibited in vivo protective effects on rapeseed leaves and tomato fruit. Notably, the succinate dehydrogenase inhibitory activities revealed that compounds 16 and 22 displayed a stronger inhibitory effect on porcine succinate dehydrogenase (SDH) with IC50 values of 1.85 and 0.39 mu mol/L, respectively, compared to Fluxapyroxad (IC50 = 5.48 mu mol/L). Molecular docking and DFT calculations have confirmed that the binding mode of compound 16 closely resembles that of Fluxapyroxad. Incorporating a conjugated alkyne motif in these compounds can enhance their binding affinity with the target protein, thereby providing a valuable structural design strategy for further developing succinate dehydrogenase inhibitors.

  • 相关文献
作者其他论文 更多>>
置顶
购物车
反馈

© 京ICP备09089781号-29 主办单位：湖北省农业科学院

学术资源： 中国农业科学院 农业专业知识服务系统 农科联盟资源共建共享平台 中国农业科技文献与信息服务平台 中国农业期刊集成服务平台