Novel promising linezolid analogues: rational design, synthesis and biological evaluation

Eur J Med Chem. 2013 Nov:69:779-85. doi: 10.1016/j.ejmech.2013.09.035. Epub 2013 Sep 25.

Abstract

A new series of 5-substituted oxazolidinones derived from linezolid, having urea and thiourea moieties at the C-5 side chain of the oxazolidinone ring, were prepared and their in vitro antibacterial activity was evaluated. The compound 10f demonstrated high antimicrobial activity, comparable to that of linezolid against Staphylococcus aureus.

Keywords: Antibacterial; Linezolid; Oxazolidinone; Structure–activity relationship; Thiourea.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetamides / chemical synthesis
  • Acetamides / chemistry
  • Acetamides / pharmacology*
  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Design*
  • Linezolid
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Oxazolidinones / chemical synthesis
  • Oxazolidinones / chemistry
  • Oxazolidinones / pharmacology*
  • Staphylococcus aureus / cytology
  • Staphylococcus aureus / drug effects*
  • Structure-Activity Relationship

Substances

  • Acetamides
  • Anti-Bacterial Agents
  • Oxazolidinones
  • Linezolid