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Novel Benzothiazole Derivatives as Potential Anti-Quorum Sensing Agents for Managing Plant Bacterial Diseases: Synthesis, Antibacterial Activity Assessment, and SAR Study.

Pan-Long ChuYu-Mei FengZhou-Qing LongWan-Lin XiaoJin JiXiang ZhouPu-Ying QiTai-Hong ZhangHeng ZhangLi-Wei LiuSong Yang
Published in: Journal of agricultural and food chemistry (2023)
As quorum sensing (QS) regulates bacterial pathogenicity, antiquorum sensing agents have powerful application potential for controlling bacterial infections and overcoming pesticide/drug resistance. Identifying anti-QS agents thus represents a promising approach in agrochemical development. In this study, the anti-QS potency of 53 newly prepared benzothiazole derivatives containing an isopropanolamine moiety was analyzed, and structure-activity relationships were examined. Compound D 3 exhibited the strongest antibacterial activity, with an in vitro EC 50 of 1.54 μg mL -1 against Xanthomonas oryzae pv oryzae ( Xoo ). Compound D 3 suppressed QS-regulated virulence factors (e.g., biofilm, extracellular polysaccharides, extracellular enzymes, and flagella) to inhibit bacterial infection. In vivo anti- Xoo assays indicated good control efficiency (curative activity, 47.8%; protective activity, 48.7%) at 200 μg mL -1 . Greater control efficiency was achieved with addition of 0.1% organic silicone or orange peel essential oil. The remarkable anti-QS potency of these benzothiazole derivatives could facilitate further novel bactericidal compound development.
Keyphrases
  • pseudomonas aeruginosa
  • staphylococcus aureus
  • escherichia coli
  • essential oil
  • high throughput
  • biofilm formation
  • transcription factor
  • climate change
  • rectal cancer
  • antimicrobial resistance
  • human health