Synthesis and biological evaluation of novel benzoxazinyl-oxazolidinones as potential antibacterial agents

Bioorg Med Chem Lett. 2013 Jul 1;23(13):3697-9. doi: 10.1016/j.bmcl.2013.05.023. Epub 2013 May 17.

Abstract

A number of benzoxazinyl-oxazolidinones bearing 3-trizolylmethyl or 3-carboxamide side chain were designed and synthesized with the aim to develop antibacterial agents with improved properties. In vitro antibacterial activities of these novel compounds were evaluated against a panel of resistant and susceptible Gram-positive bacteria. Most analogues bearing 3-trizolylmethyl showed good to moderate antibacterial activities. Compound 12a exhibited a fourfold increase in activity compared with linezolid against all the tested strains, which was identified to be a promising antibacterial agent for further evaluation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology*
  • Benzoxazines / chemistry
  • Benzoxazines / pharmacology*
  • Dose-Response Relationship, Drug
  • Gram-Positive Bacteria / drug effects*
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Oxazolidinones / chemistry
  • Oxazolidinones / pharmacology*
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Benzoxazines
  • Oxazolidinones