Designing Biaryl Pyrazole Derivatives for Antibacterial Activity against Plant Pathogenic Bacteria

  • J Agric Food Chem. 2026 Jun 10;74(22):16919-16931. doi: 10.1021/acs.jafc.5c14546.
Qi Li  1  2 ,  Xiaoyu Pan  1  2 ,  Hongbo Duan  1  2 ,  Jiuhui Ye  1  2 ,  Yizhou Yang  1  2 ,  Qin Peng  1 ,  Xiuhuan Li  3 ,  Zhiqing Ma  1  2 ,  He Yan  1  2 ,  Xili Liu  1
Affiliations
  • 1. College of Plant Protection, Northwest A&F University, Yangling, Shaanxi 712100, People's Republic of China.
  • 2. Engineering and Technology Centers of Biopesticide in Shaanxi, Yangling, Shaanxi 712100, People's Republic of China.
  • 3. State Key Laboratory for Crop Stress Resistance and High-Efficiency Production, Northwest A&F University, Yangling, Shaanxi 712100, People's Republic of China.
PMID: 42223285 DOI: 10.1021/acs.jafc.5c14546
Abstract

Plant Bacterial diseases severely threaten global agricultural production. In this study, a series of biaryl pyrazole derivatives (Series I-III) were synthesized and evaluated for their activity against five major phytopathogens, including Xanthomonas oryzae pv. oryzae (Xoo), Pseudomonas syringae pv. actinidiae (Psa), Xanthomonas citri subsp. citri (Xcc), Acidovorax citrulli (Ac), and Ralstonia solanacearum (Rs). Among them, compound II-28 exhibited potent broad-spectrum Antibacterial activity, with an MIC value as low as 12.5 μg/mL. In vivo trials demonstrated that II-28 effectively controlled rice Bacterial blight and kiwifruit canker, performing comparably to thiodiazole copper. Preliminary mechanistic studies suggested that II-28 may target the LolCDE complex, modulates the expression of relevant genes, disrupts lipoprotein transport, and inhibits Bacterial division. This work identifies biaryl pyrazoles as promising bactericidal leads and suggests LolCDE as a potential novel target for managing plant Bacterial diseases.

Keywords
LolCDE complex inhibitors; agricultural bactericides; biaryl pyrazole derivatives; phytopathogenic bacteria.
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