Journal
PESTICIDE BIOCHEMISTRY AND PHYSIOLOGY
Volume 156, Issue -, Pages 160-169Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.pestbp.2019.02.017
Keywords
1,2,3-triazole; Succinate dehydrogenase inhibitors; Fungicidal activity; Molecular docking simulation
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Funding
- National Key Research and Development Program of China [2017YFD0200506]
- National Natural Science Foundation of China [31572043]
- Jiangsu Agriculture Science and Technology Innovation Fund [CX(18)3055]
- Natural Science Foundation of Jiangsu Province [BK20151428]
- Qing Lan Project of Jiangsu Province
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Succinate dehydrogenase (SDH) is demonstrably one of the most important molecular targets in development of new fungicide. In our continuous efforts to discover novel SDH inhibitors, forty-two carboxamide derivatives containing 1,2,3-triazole ring were designed and synthesized, which were precisely characterized by H-1 NMR, ESI-MS, elemental analysis and X-ray single-crystal diffraction. The compounds were screened for antifungal activities against phytopathogenic fungi by mycelia growth inhibition assay in vitro. Compound A3-3 exhibited significant antifungal activity against Sclerotinia sclerotiorum, Botrytis cinerea, Rhizoctonia cerealis and Gaeumannomyces graminsis with EC50 values of 1.08, 8.75, 1.67 and 5.30 mu g/mL, respectively, comparable to those of commercial SDHI boscalid. In vivo testing demonstrated that A3-3 was effective for suppressing rape sclerotinia rot, cucumber grey mould and wheat powdery mildew caused by S. sclerotiorum, B. cinerea and Blumeria gramirtis at a dosage of 200 mu g/mL. Inhibition activities against SDH test proved the designed analogues were effective in the enzyme level. The molecular docking simulation revealed that A3-3 interacted with ARG43, TYR58 and TRP173 of the SDH through hydrogen bond and pi-pi interaction, which could explain the probable mechanism of action between the inhibitor and target protein.
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