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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
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Published on: June 23, 2019

Designing Biaryl Pyrazole Derivatives for Antibacterial Activity against Plant Pathogenic Bacteria.

Qi Li1,2, Xiaoyu Pan1,2, Hongbo Duan1,2

  • 1College of Plant Protection, Northwest A&F University, Yangling, Shaanxi 712100, People's Republic of China.

Journal of Agricultural and Food Chemistry
|June 1, 2026
PubMed
Summary

New biaryl pyrazole compounds show strong antibacterial activity against major plant pathogens. Compound II-28 effectively controls rice bacterial blight and kiwifruit canker, offering a promising new strategy for disease management.

Keywords:
LolCDE complex inhibitorsagricultural bactericidesbiaryl pyrazole derivativesphytopathogenic bacteria

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Published on: October 1, 2015

Area of Science:

  • Agricultural Science
  • Organic Chemistry
  • Plant Pathology

Background:

  • Plant bacterial diseases pose significant threats to global food security.
  • Developing novel, effective bactericides is crucial for sustainable agriculture.

Purpose of the Study:

  • To synthesize and evaluate novel biaryl pyrazole derivatives for antibacterial activity against key plant pathogens.
  • To identify potent bactericidal compounds and explore their mechanism of action.

Main Methods:

  • Synthesis of biaryl pyrazole derivatives (Series I-III).
  • In vitro evaluation of antibacterial activity against Xanthomonas oryzae pv. oryzae (Xoo), Pseudomonas syringae pv. actinidiae (Psa), Xanthomonas citri subsp. citri (Xcc), Acidovorax citrulli (Ac), and Ralstonia solanacearum (Rs).
  • In vivo efficacy trials on rice bacterial blight and kiwifruit canker.
  • Preliminary mechanistic studies on compound II-28.

Main Results:

  • Compound II-28 demonstrated potent broad-spectrum activity with a minimum inhibitory concentration (MIC) as low as 12.5 μg/mL.
  • II-28 effectively controlled rice bacterial blight and kiwifruit canker in vivo, comparable to thiodiazole copper.
  • Mechanistic studies indicated II-28 may target the LolCDE complex, affecting lipoprotein transport and bacterial division.

Conclusions:

  • Biaryl pyrazoles represent a promising class of bactericidal agents for plant disease management.
  • The LolCDE complex is identified as a potential novel target for developing new antibacterial strategies in agriculture.