Rice bacterial leaf blight is a destructive bacterial disease caused byXanthomonas oryzae pv. oryzae(Xoo) that seriously threatens crop yields and their associated economic benefits. In this study, a series of improved dissolubility 7-aliphatic amine tryptanthrin derivatives was designed and synthesized, and their potency in antibacterial applications was investigated. Notably, compound6eexhibited excellent activity againstXoo, with an EC50value of 2.55 μg/mL, compared with the positive control bismerthiazol (EC50= 35.0 μg/mL) and thiodiazole copper (EC50= 79.4 μg/mL). In vivo assays demonstrated that6eexhibited a significant protective effect on rice leaves. After exposure, the morphology of the bacteria was partially atrophied by SEM. Furthermore,6eincreased the accumulation of intracellular reactive oxygen species, causing cell apoptosis and the formation of bacterial biofilms. All the results indicated that6ecould be a potential agrochemical bactericide for controlling phytopathogenic bacteria.