Oxazolidinones - A review

The oxazolidinones represent a novel chemical class of synthetic antimicrob ial agents. They exhibit an unique mechanism of protein synthesis inhibitio n and generally display bacteriostatic activity against many important huma n pathogens, including methicillin-resistant Staphylococcus aureus, vancomy cin-resistant enterococci, and penicillin- and cephalosporin-resistant Stre ptococcus pneumoniae. Linezolid, the oxazolidinone which has been selected for clinical development, has near complete oral bioavailability plus favou rable pharmacokinetic and toxicity profiles. Results from experimental mode ls of infection and phase II trials reveal linezolid to be highly active in vivo against infections due to many common Gram-positive pathogens. The ro le of linezolid remains to be determined in phase III clinical trials, but it shows great promise as an alternative to glycopeptides and streptogramin s to treat serious infections due to resistant Gram-positive organisms. Fur ther modification of the oxazolidinone nucleus may yield agents with even g reater potency and with novel spectra of activity.