Xanthomonas oryzae pv. oryzae (Xoo) is an offensive phytopathogen that can invade a wide range of plant hosts to develop bacterial diseases, including the well-known rice bacterial leaf blight. However, few agrochemicals have been identified to effectively prevent and eliminate Xoo-induced diseases. Thus, designing novel antibacterial compounds on the basis of the potential targets from Xoo may lead to the discovery of highly efficient and innovative anti-Xoo agents. Filamentous temperature-sensitive protein Z (FtsZ), an important functional protein in the progression of cell division, has been widely reported and exploited as a target for creating antibacterial drugs in the field of medicine. Therefore, the fabrication of innovative frameworks targeting XooFtsZ may be an effective method for managing bacterial leaf blight diseases via blocking the binary division and reproduction of Xoo. As such, a series of novel N-(cinnamoyl)-N′-(substituted)acryloyl hydrazide derivatives containing pyridinium moieties were designed, and the anti-Xoo activity was determined. The bioassay results showed that compound A7 had excellent anti-Xoo activity (EC50 = 0.99 mg L–1) in vitro and distinct curative activity (63.2% at 200 mg L–1) in vivo. Further studies revealed that these designed compounds were XooFtsZ inhibitors, validating by the reduced GTPase activity of recombinant XooFtsZ, the nonfilamentous XooFtsZ assembly observed in the TEM images, and the prolonged Xoo cells from the fluorescence patterns. Computational docking studies showed that compound A7 had strong interactions with ASN34, GLN193, and GLN197 residues located in the α helix regions of XooFtsZ. The present study demonstrates the developed FtsZ inhibitors can serve as agents to control Xoo-induced infections.
1,2,4-Thiadiazole derivatives containing a sulfone moiety were designed and synthesized via scaffold hopping to facilitate the discovery of novel antibacterial agents. Most of the compounds exhibited excellent activity against three plant pathogenic bacteria. The half-maximal effective concentrations (EC50) of compound B7 for Xanthomonas oryzae pv oryzae (Xoo) and X. oryzae pv oryzicola (Xoc) concentrations were 0.4 and 1.0 mg/L, respectively. In addition, the EC50 values of compounds B1 and B24 for Xoo, Xoc, and Pseudomonas syringae pv actinidiae (Psa) were less than 5 mg/L and significantly better than those of the positive control agents thiodiazole copper (121.8, 119.5, and 142.0 mg/L, respectively) and bismerthiazol (73.3, 65.6, and 128.8 mg/L, respectively). Compound B7 exhibited protective and curative activities of 48.1 and 46.7%, respectively, against bacterial leaf blight, which were higher than those of bismerthiazol (35.5 and 36.9%, respectively) and thiodiazole copper (39.3 and 39.5%, respectively). Additionally, compound B7 exerted an effect on the virulence factors of Xoo (production of exopolysaccharides and extracellular enzymes, biofilm formation, and motility), membrane permeability, cell surface morphology, and intracellular content of reactive oxygen species. Transcriptome analysis showed that compound B7 improved the resistance of rice plants to external stress by influencing the metabolic process, biological regulation, catalytic activity of enzymes, and plant–pathogen interaction. Compound B7 can therefore be considered as a potential candidate antibacterial agent and warrants an in-depth investigation in the future.
危险品化学品经营许可证（带存储）