Synthesis and Antimicrobial Studies of Coumarin-Substituted Pyrazole Derivatives as Potent Anti- Staphylococcus aureus Agents

Molecules. 2020 Jun 15;25(12):2758. doi: 10.3390/molecules25122758.

Abstract

In this paper, synthesis and antimicrobial studies of 31 novel coumarin-substituted pyrazole derivatives are reported. Some of these compounds have shown potent activity against methicillin-resistant Staphylococcus aureus (MRSA) with minimum inhibitory concentration (MIC) as low as 3.125 µg/mL. These molecules are equally potent at inhibiting the development of MRSA biofilm and the destruction of preformed biofilm. These results are very significant as MRSA strains have emerged as one of the most menacing pathogens of humans and this bacterium is bypassing HIV in terms of fatality rate.

Keywords: MRSA; S. epidermidis; Staphylococcus aureus; antimicrobial; biofilm; coumarin; hydrazone; pyrazole.

MeSH terms

  • Anti-Bacterial Agents / pharmacology
  • Anti-Infective Agents
  • Biofilms / drug effects
  • Coumarins / chemical synthesis*
  • Coumarins / metabolism
  • Coumarins / pharmacology
  • Methicillin-Resistant Staphylococcus aureus / drug effects
  • Microbial Sensitivity Tests
  • Pyrazoles / metabolism
  • Pyrazoles / pharmacology
  • Staphylococcal Infections / microbiology
  • Staphylococcus aureus / drug effects*

Substances

  • Anti-Bacterial Agents
  • Anti-Infective Agents
  • Coumarins
  • Pyrazoles
  • pyrazole
  • coumarin