Oxazolidinones--a new class of broad-spectrum chemotherapeutics.

Abstract

The oxazolidinones are a new class of broad spectrum chemotherapeutics of antibiotic properties. These drugs have good activity against Gram-positive pathogenic bacteria. Oxazolidinones possess an unique mechanism of inhibitory bacterial protein biosynthesis. These compounds inhibit the formation of N-formylmethionyl-tRNA, which is a requisite of beginning translation process. Linezolid, the first oxazolidinone to be approved for the clinical treatment of Gram-positive bacterial infections, displays a wide spectrum of in vitro activity against many important pathogens, including for instance methicillin-resistant Staphylococcus aureus, vancomycin-resistant enterococci and penicillin-resistant pneumococci. Linezolid is a pararental drug that also possesses near-complete oral bioavailability and a favourable pharmacokinetic profile. In clinical trials involving hospitalised patients with skin and soft tissue infections oxazolidinones appeared to be effective treatment option, comparable in efficacy to vancomycin.