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Article Abstract
Background: Pongamol is a flavonoid natural product containing a 1,3-dicarbonyl structure, which has various biological activities and plays an important role as the main skeleton in new drug development. 1,3-dicarbonyl compounds are not only widely used as synthetic building blocks in many organic reactions, but also commonly found in natural products and active molecules in pharmaceuticals. Sixty-one dicarbonyl derivatives were designed and synthesized using the 1,3-dicarbonyl active fragment as a structural unit and their antifungal activities against six agricultural plant pathogens were determined. The compound ET-17 with the most significant activity against Botrytis cinerea was finally selected to study its preliminary mechanism of action.
Results: Most fluorinated compounds exhibited significant antimicrobial activities against fungi. Among them, compounds ET-6, ET-17, EFM-6, EFM-7, EFM-8, BZ-11 and BZ-12 exhibited remarkable antifungal activity in vitro against plant pathogenic fungi. Especially, compound ET-17 displayed the broad-spectrum antifungal activities against Botrytis cinerea, Fusarium graminearum, Rhizoctonia solani, Sclerotinia sclerotiorum, Fusarium oxysporum and Phytophthora capsici with EC values of 0.740, 0.635, 0.640, 1.732, 4.515 and 1.984 μg/mL, respectively. Further mechanism research results indicated that compound ET-17 might cause mycelial abnormality, cell membrane breakage, accumulation of reactive oxygen species (ROS) of B. cinerea to inhibit mycelial growth. Furthermore, the in vivo protection experiments showed that compound ET-17 had a certain protective effect (72.23%) at 100 μg/mL.
Conclusion: The 1,3-dicarbonyl derivatives showed efficient and broad-spectrum antifungal activities against six plant pathogens, which is expected to become a new broad-spectrum bactericidal candidate for controlling plant diseases. © 2025 Society of Chemical Industry.
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Background: Pongamol is a flavonoid natural product containing a 1,3-dicarbonyl structure, which has various biological activities and plays an important role as the main skeleton in new drug development. 1,3-dicarbonyl compounds are not only widely used as synthetic building blocks in many organic reactions, but also commonly found in natural products and active molecules in pharmaceuticals. Sixty-one dicarbonyl derivatives were designed and synthesized using the 1,3-dicarbonyl active fragment as a structural unit and their antifungal activities against six agricultural plant pathogens were determined.
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