Synthesis and antimicrobial studies of novel derivatives of 4-(4-formyl-3-phenyl-1H-pyrazol-1-yl)benzoic acid as potent anti-Acinetobacter baumannii agents

Bioorg Med Chem Lett. 2017 Feb 1;27(3):387-392. doi: 10.1016/j.bmcl.2016.12.068. Epub 2016 Dec 29.

Abstract

Microbial resistance to antibiotics is a global concern. The World Health Organization (WHO) has identified antimicrobial resistance as one the three greatest threats for human beings in the 21st century. Without urgent and coordinated action, the world is moving toward a post-antibiotic era, in which normal infections or minor injuries may become fatal. In an effort to find new agents, we report the synthesis and antimicrobial activities of 40 novel 1,3-diphenyl pyrazole derivatives. These compounds have shown zones of growth inhibition up to 85mm against Acinetobacter baumannii. We tested the active compounds against this Gram-negative bacterium in minimum inhibitory concentration (MIC) tests and found activity with concentration as low as 4μg/mL.

Keywords: Acinetobacter baumannii; Antibacterial; Antimicrobials; Hydrazone; Methicillin-resistant Staphylococcus aureus (MRSA); Pyrazole; Resistant.

MeSH terms

  • Acinetobacter baumannii / drug effects
  • Acinetobacter baumannii / enzymology
  • Anti-Infective Agents / chemical synthesis*
  • Anti-Infective Agents / chemistry
  • Anti-Infective Agents / pharmacology
  • Benzoic Acid / chemical synthesis
  • Benzoic Acid / chemistry*
  • Benzoic Acid / pharmacology
  • Binding Sites
  • Catalytic Domain
  • Drug Resistance, Multiple, Bacterial / drug effects
  • Gram-Negative Bacteria / drug effects
  • Gram-Positive Bacteria / drug effects
  • Microbial Sensitivity Tests
  • Molecular Docking Simulation
  • Pyrazoles / chemistry*
  • Structure-Activity Relationship

Substances

  • Anti-Infective Agents
  • Pyrazoles
  • pyrazole
  • Benzoic Acid