Discovery of Highly Efficient Novel Potential Succinate Dehydrogenase Inhibitors Containing a Stilbene Group for Management of Sheath Blight of Rice and Sclerotinia Stem Rot of Oilseed Rape
In the search for novel succinate dehydrogenase inhibitors (SDHIs) fungicides for managing rice sheath blight (RSB) and sclerotinia stem rot (SSR), 28 pyrazole-4-carboxamides incorporating stilbene or diphenylacetylene scaffolds were synthesized and evaluated for antifungal activities. The results showed that compound <b>7m</b> exhibited the most promising antifungal efficacy against <i>Rhizoctonia solani</i> and <i>Sclerotinia sclerotiorum</i> with EC<sub>50</sub> (half maximal effective concentration) values of 0.004 and 0.028 μg/mL, outperforming Boscalid and Fluxapyroxad. Furthermore, the detached leaf assay showed that <b>7m</b> showed remarkable protective and curative efficacies against <i>R. solani</i> and significant inhibition of <i>S. sclerotiorum</i> growth on oilseed rape leaves, indicating that it had a promising application prospect for RSB and SSR management. Further SDH enzymatic inhibition assay, scanning electron microscopy (SEM), molecular docking studies, and molecular dynamics (MD) simulations revealed that compound <b>7m</b> shared an antifungal mechanism similar to that of Fluxapyroxad, which was further validated by density functional theory (DFT) and electrostatic potential (ESP) calculations. These findings suggested that <b>7m</b> held significant promise as a novel SDHI for the effective management of RSB and SSR, warranting further investigation.
Authors
- Kun Fang (ORCID: https://orcid.org/0000-0002-1209-349X)
- Xinyi Liu (ORCID: https://orcid.org/0000-0002-1645-9428)
- Bo Luo (ORCID: https://orcid.org/0000-0001-8519-4446)
- Yanbing Wu (ORCID: https://orcid.org/0000-0002-4569-1015)
- Fengjia Zhang
- Qingsi Zhang
- Rongrong Li (ORCID: https://orcid.org/0000-0001-7094-6289)
- Miao Wang (ORCID: https://orcid.org/0000-0002-1607-0666)
- Rong Wang (ORCID: https://orcid.org/0000-0002-5108-3286)
- Yu-Qing Guo
- Mengxing Liu
- Mengnan Zhou
Institutions
- Xinyang Normal University (CN)
- Institute of Food Science & Technology (GB)
- Tea Research Institute (CN)
- Rocky Mountain Research (United States) (US)
- Northwest A&F University (CN)
Publication Details
- Journal
- Journal of Agricultural and Food Chemistry
- Published
- 2025-09-09
- DOI
- https://doi.org/10.1021/acs.jafc.5c03978
- Primary Topic
- Fungal Plant Pathogen Control
- Type
- article
- Field-Weighted Citation Impact
- 0.00