Design and Synthesis of Malonamide Derivatives as Antibiotics against Methicillin-Resistant Staphylococcus aureus

Molecules. 2017 Dec 22;23(1):27. doi: 10.3390/molecules23010027.

Abstract

Methicillin-resistant Staphylococcus aureus (MRSA) is a serious threat to humans. Most existing antimicrobial drugs, including the β-lactam and quinoxiline classes, are not effective against MRSA. In this study, we synthesized 24 derivatives of malonamide, a new class of antibacterial agents and potentiators of classic antimicrobials. A derivative that increases bacterial killing and biofilm eradication with low cell toxicity was created.

Keywords: Staphylococcus aureus; antibiotics; malonamide.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / pharmacology
  • Biofilms / drug effects*
  • Biofilms / growth & development
  • Cyclopropanes / chemistry*
  • Dicarboxylic Acids / chemistry*
  • Drug Design
  • Humans
  • Malonates / chemical synthesis*
  • Malonates / pharmacology
  • Methicillin-Resistant Staphylococcus aureus / drug effects*
  • Methicillin-Resistant Staphylococcus aureus / growth & development
  • Methicillin-Resistant Staphylococcus aureus / isolation & purification
  • Microbial Sensitivity Tests
  • Staphylococcal Infections / microbiology
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Cyclopropanes
  • Dicarboxylic Acids
  • Malonates
  • malonamide