Fungicidal activity of novel quinazolin‐6‐ylcarboxylates and mode of action on Botrytis cinerea

Abstract

BACKGROUND Fungal diseases remain important causes of crop failure and economic losses. As the resistance toward current selective fungicides becomes increasingly problematic, it is necessary to develop efficient fungicides with novel chemotypes. RESULTS A series of novel quinazolin‐6‐ylcarboxylates which combined the structures of pyridine or heterocyclic motif and the N‐(3‐chloro‐4‐fluorophenyl)quinazolin‐4‐amine moiety, a binding group of ATP‐binding site of gefitinib, were evaluated for their fungicidal activity on different phytopathogenic fungi. Most of these compounds showed excellent fungicidal activities against Botrytis cinerea and Exserohilum rostratum, especially compound F17 displayed the highest activity with EC50 values as 3.79 μg mL−1 against B. cinerea and 2.90 μg mL−1 against E. rostratum, which was similar to or even better than those of the commercial fungicides, such as pyraclostrobin (EC50, 3.68, 17.38 μg mL−1) and hymexazol (EC50, 4.56, 2.13 μg mL−1). Moreover, compound F17 significantly arrested the lesion expansion of B. cinerea infection on tomato detached leaves and strongly suppressed grey mold disease on tomato seedlings in greenhouse. The abilities of compound F17 to induce cell apoptosis of the non‐germinated spores, to limit oxalic acid production, to reduce malate dehydrogenase (MDH) expression, and to block the active pocket of MDH protein were demonstrated in B. cinerea. CONCLUSION The novel quinazolin‐6‐ylcarboxylates containing ATP‐binding site‐directed moiety, especially compound F17, could be developed as a potential fungicidal candidate for further study. © 2023 Society of Chemical Industry.

Evaluation of Equisetin as an Anti-Microbial and Herbicidal Agent from Endophytic Fungus Fusarium sp. JDJR1

“…Each treatment was repeated three times and cultivated at 25 • C for 24 h. A small hole was pricked in the tomato fruit with a sterile needle, and the activated pathogenic fungal cake was inoculated into the pricked hole. After cultivating in the dark at 25 • C for 72 h, the diameter of the lesion was measured and the inhibition rate was calculated using the same formula in [29].…”

Design, Synthesis, and Antifungal Evaluation of Diverse Heterocyclic Hydrazide Derivatives as Potential Succinate Dehydrogenase Inhibitors

“…Pathogenic fungi infections are one of the most destructive plant diseases that can significantly reduce the quality and yield of food crops. − Most of the existing fungicides can achieve control of pathogenic fungi, but as a result of long-term unreasonable use, pathogenic fungi have developed serious drug resistance. In addition, some commercial products displayed side effects to the beneficial microorganisms.…”

Colour-analyzer: a new dual colour model-based imaging tool to quantify plant disease

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