[Modification of novel oxazolidinone derivatives at C-5 side chain and their antibacterial activities]

Yao Xue Xue Bao. 2006 Oct;41(10):985-9.
[Article in Chinese]

Abstract

Aim: To modify the C-5 side chains of the oxazolidinone derivatives and evaluate their in vitro antibacterial activities preliminarily.

Methods: The title compounds were synthesized in 9 - 12 steps with the starting material 3-fluoroaniline and their in vitro antibacterial activities were examined by using Mueller-Hinton broth dilution method.

Results: Thirty new compounds were designed and synthesized, in which eighteen novel title compounds were prepared and their structures were confirmed by 1H NMR and ESI-MS. Eleven compounds showed antibacterial activities to a certain extent, among them compounds 7a, 9a and 11a displayed promising activity.

Conclusion: Compounds 7a, 9a and 11a were worth further studying.

Publication types

  • English Abstract

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Oxazolidinones / chemical synthesis*
  • Oxazolidinones / chemistry
  • Oxazolidinones / pharmacology
  • Staphylococcus aureus / drug effects
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Oxazolidinones