Novel Diphenyl Ether Carbonyl Ester Fragment as a Promising Skeleton Targeting Succinate Dehydrogenase

作者：Yanhao Hu, Zhengxi Xiong, Mian Wei, Ping Chen, Xu He, Xianghui Luo, Hafiz Muhammad Usama Shaheen, Wei Yan, Yonghao Ye, Bo He · 发表于：Journal of Agricultural and Food Chemistry · 年份：2025 · DOI：10.1021/acs.jafc.5c02499 · 被引用次数：10 · 研究领域：Enzyme Catalysis and Immobilization、Enzyme function and inhibition、Microbial metabolism and enzyme function

Succinate dehydrogenase (SDH) is a globally recognized critical target for fungicides. Our research mainly focuses on discovering novel molecular skeletons targeting SDH. We designed a series of diphenyl ether ester derivatives that exhibit potential efficacy against Rhizoctonia solani by utilizing a bioisosteric approach. These results indicate that compounds with shorter linkers significantly enhance the antifungal activity. Furthermore, the antifungal potential of an ester-linked compound was superior to its amide and N -(alkoxy) counterparts. Specifically, compound ba achieved a remarkable 92% efficacy in controlling R. solani at a dosage of 50 μg/mL with an EC 50 value of 0.44 μg/mL, thus outperforming boscalid without negatively impacting rice growth. Moreover, ba caused significant damage to the R. solani mycelium and demonstrated an IC 50 value of 1.69 μM against R. solani SDH, exhibiting efficacy comparable to that of boscalid. These results unveil a promising avenue for replacing traditional heterocyclic amide-based inhibitors, potentially heralding a new generation of SDH-targeting fungicides.