Antibacterial activity of new oxazolidin-2-one analogues in methicillin-resistant Staphylococcus aureus strains

Int J Mol Sci. 2014 Mar 26;15(4):5277-91. doi: 10.3390/ijms15045277.

Abstract

Staphylococcus aureus is one of the most common causes of nosocomial infections. The purpose of this study was the synthesis and in vitro evaluation of antimicrobial activity of 10 new 3-oxazolidin-2-one analogues on 12 methicillin resistant S. aureus (MRSA) clinical isolates. S. aureus confirmation was achieved via catalase and coagulase test. Molecular characterization of MRSA was performed by amplification of the mecA gene. Antimicrobial susceptibility was evaluated via the Kirby-Bauer disc diffusion susceptibility test protocol, using commonly applied antibiotics and the oxazolidinone analogues. Only (R)-5-((S)-1-dibenzylaminoethyl)-1,3-oxazolidin-2-one (7a) exhibited antibacterial activity at 6.6 μg. These results, allow us to infer that molecules such as 7a can be potentially used to treat infections caused by MRSA strains.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / adverse effects
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / pharmacology*
  • Artemia / drug effects
  • Bacterial Proteins / genetics
  • Disk Diffusion Antimicrobial Tests
  • Drug Resistance, Multiple, Bacterial
  • Methicillin-Resistant Staphylococcus aureus / drug effects*
  • Oxazolidinones / adverse effects
  • Oxazolidinones / chemical synthesis
  • Oxazolidinones / pharmacology*
  • Penicillin-Binding Proteins
  • Protein Synthesis Inhibitors / adverse effects
  • Protein Synthesis Inhibitors / chemical synthesis
  • Protein Synthesis Inhibitors / pharmacology
  • Staphylococcal Infections / drug therapy*
  • beta-Lactam Resistance / genetics

Substances

  • Anti-Bacterial Agents
  • Bacterial Proteins
  • Oxazolidinones
  • Penicillin-Binding Proteins
  • Protein Synthesis Inhibitors
  • mecA protein, Staphylococcus aureus