Data · dataset · 2026
Discovery of a trans-Configured Monofluoroalkene as a Potent Succinate Dehydrogenase Inhibitor against Phakopsora pachyrhizi
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A series of monofluoroalkene derivatives were designed and synthesized as succinate dehydrogenase inhibitors (SDHIs).
Description
Most compounds showed high <i>in vitro</i> activity against Rhizoctonia solani, with EC<sub>50</sub> values below 0.01 mg/L. Compound <b>V-17b</b> (4-OPh) was the most potent (EC<sub>50</sub> = 0.0029 mg/L), surpassing boscalid and fluxapyroxad by over 10-fold. Several compounds retained >50% inhibition <i>in vivo</i> at 200 mg/L against Rhizoctonia solani.
Compound <b>V-6b</b> exhibited 100% efficacy against Phakopsora pachyrhizi at 1 mg/L, and <b>V-9b</b> showed 77.8% and 96.3% efficacy against Puccinia glumarum and Puccinia sorghi at 10 mg/L, respectively. Enzyme assays revealed that <b>V-9b</b> inhibited porcine SDH (IC<sub>50</sub> = 1.87 μM) more effectively than fluxapyroxad (IC<sub>50</sub> = 8.13 μM), with the <i>trans</i> isomer superior to the <i>cis</i>. Molecular docking indicated that the <i>trans</i> configuration enables additional π–π stacking with Trp_B173.
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These results demonstrate that the monofluoroalkene scaffold, combined with appropriate substitution patterns and configuration, can generate potent SDHIs with promising fungicidal profiles.
Links
Where it is published
- DOI doi.org/10.1021/acs.jafc.6c02371.s001 ↗
DOI / persistent id · from zivahub uct ac za
Catalogue records · 1
- OAI-PMH record api.figshare.com/v2/oai?verb=GetRecord&metadataPrefix=oai_dc&identifier=oai%3Af… ↗
metadata API · from zivahub uct ac za
Topics
- From keywords
- Chemistry · Earth & Environmental Science · Life Sciences · Medicine & Health
- Inferred from text
- Medicinal and biomolecular chemistry 69%
Provenance · 1 source records, 10 field assertions
| Source | Key | Last seen | Raw |
|---|---|---|---|
| ZivaHub | oai:figshare.com:article/34027403 | 11 d ago | JSON v1 |
| Field | Assertion | Extractor | Evidence |
|---|---|---|---|
| access_level | source · zivahub uct ac za | connector:zivahub_uct_ac_za@1.0.0 | |
| concepts[field].anzsrc:group:3404 | enrichment · zivahub uct ac za | taxonomy-embedding@1.1.0 | title+keywords+description (69%) |
| concepts[field].local:field:chemistry | mapping · zivahub uct ac za | connector:zivahub_uct_ac_za@1.0.0 | |
| concepts[field].local:field:earth-environmental | mapping · zivahub uct ac za | connector:zivahub_uct_ac_za@1.0.0 | |
| concepts[field].local:field:life-sciences | mapping · zivahub uct ac za | connector:zivahub_uct_ac_za@1.0.0 | |
| concepts[field].local:field:medicine-health | mapping · zivahub uct ac za | connector:zivahub_uct_ac_za@1.0.0 | |
| description | source · zivahub uct ac za | connector:zivahub_uct_ac_za@1.0.0 | /metadata/dc/description |
| license | source · zivahub uct ac za | connector:zivahub_uct_ac_za@1.0.0 | /metadata/dc/rights |
| publication_date | source · zivahub uct ac za | connector:zivahub_uct_ac_za@1.0.0 | |
| title | source · zivahub uct ac za | connector:zivahub_uct_ac_za@1.0.0 | /metadata/dc/title |