Background: With the long-term use of traditional bactericides and antiviral agents, drug resistance has become increasingly prominent, resulting in impaired crop growth and yields. Based on this, the introduction of small molecular active groups into natural products has become the direction of research for green pesticides.Results: In this study, novel 1,3,4-oxadiazole sulfonate/carboxylate flavonoid derivatives were explored. Among them, D4 exhibited good inhibitory effects on plant bacteria. It is worth mentioning that D4 (15 ∼g ml −1 ) exhibited an excellent median effective concentration (EC 50 ) value against Xanthomonas oryzae pv. oryzae (Xoo), which was better than bismerthiazol (73 ∼g ml −1 ) and thiodiazole copper (100 ∼g ml −1 ). The EC 50 for D4 was much lower than the two positive controls (bismerthiazol, thiodiazole copper), making D4 more potent in this assay of bacterial growth inhibition. In addition, mechanism research using scanning electron microscopy revealed that D4 could cause deformation or rupture of the cell membranes of Xoo and Pseudomonas syringae pv. actinidiae. Moreover, D4 exhibited the best EC 50 for in vivo curative (132 ∼g ml −1 ) and protective (101 ∼g ml −1 ) activities against tobacco mosaic virus, which were more effective than ningnanmycin. Microscale thermophoresis data suggested that D4 [dissociation constant (K d ) = 0.038 ± 0.011 ∼mol L −1 ] exhibited a stronger binding capacity than the control agent ningnanmycin (K d = 4.707 ± 2.176 ∼mol L −1 ).
Conclusion:The biological activity data and mode of action demonstrated that D4 had the best antibacterial and antiviral effects. Compound D4 discovered in the current work may be a very promising agricultural drug.