Design, Synthesis, and Biological Evaluation of Novel Quinoline Derivatives against Phytopathogenic Bacteria Inspired from Natural Quinine Alkaloids.

A series of 2-(trifluoromethyl)-4-hydroxyquinoline derivatives were designed and synthesized with introduction of the antibacterial fragment amino alcohols, and their antibacterial activity against plant phytopathogenic bacteria was evaluated for the development of quinoline bactericides. It is worth noting that compound exhibited excellent antibacterial activity with a minimum inhibitory concentration (MIC) value of 3.12 μg/mL against (). Furthermore, assays demonstrated that the protective efficacy of against rice bacterial blight at 200 μg/mL (33.0%) was superior to that of the commercial agent bismerthiazol (18.3%), while the curative efficacy (35.0%) was comparable to that of bismerthiazol (35.7%). The antibacterial mechanisms of indicated that it affected the activity of bacteria by inducing intracellular oxidative damage in and disrupting the integrity of the bacterial cell membrane. The above results demonstrated that the novel quinoline derivative possessed excellent and antibacterial activity, indicating its potential as a novel green agricultural antibacterial agent.