Oxazolidinone Antibacterial Agents

Abstract

The oxazolidinones are a new class of synthetic antibacterial agents. These compounds demonstrate potent in vitro and in vivo activity against important human pathogens, including multiple antibiotic-resistant strains of gram positive organisms including the staphylococci, streptococci, and enterococci. The oxazolidinones have a novel mechanism of action, inhibiting bacterial protein synthesis at a very early step prior to initiation. Literature disclosures have described the inability to detect in vitro bacterial resistance development to the oxazolidinones. Only the (S)-enantiomer is active; a new synthetic route yielding oxazolidinones with high optical purity has been reported. This paper will review the spectrum of activity, mechanism of action studies, toxicity issues, and structure activity relationships of the oxazolidinones.