Background Xanthomonas oryzae pv. oryzae ( Xoo ) can cause destructive bacterial leaf blight in rice. As an antibacterial, resveratrol may inhibit Xoo growth. This study focused on the potential structural-activity relationship of resveratrol and its derivatives against Xoo growth, and 1 H-NMR-based metabolomic analysis was applied to investigate the global metabolite changes in Xoo after resveratrol treatment.Results Resveratrol showed the strongest inhibitory effects on Xoo growth compared with its derivatives, which lacked double bonds (compounds 4 – 6 ) or hydroxyls were substituted with methoxyls (compounds 7 – 9 ). The IC 50 of resveratrol against Xoo growth was 11.67 ± 0.58 μg/mL. Results indicated that the double bond of resveratrol contributed to its inhibitory effects on Xoo growth, and hydroxyls were vital for this inhibition. Interestingly, resveratrol also significantly inhibited Xoo flagellum growth. Based on 1 H-NMR global metabolic analysis, a total of 30 Xoo metabolites were identified, the changes in the metabolic profile indicated that resveratrol could cause oxidative stress as well as disturb energy, purine, amino acid, and NAD + metabolism in Xoo , resulting in the observed inhibitory effects on growth.Conclusions This study showed that the double bond of resveratrol contributed to its inhibitory effects on Xoo growth, and hydroxyls were also the important active groups. Resveratrol could cause oxidative stress of Xoo cells, and disturb the metabolism of energy, purine, amino acid and NAD +, thus inhibit Xoo growth.