Oxazolidinone Antibacterials and Our Experience

The Oxazolidinones are a promising novel chemical synthetic class of antibiotics identified in the last two decades and have been subjected to intensive discovery efforts. They possess impressive antibacterial activity against Grampositive pathogens. Oxazolidinones act through a unique mechanism of inhibitory bacterial protein biosynthesis. Linezolid (ZyvoxTM) has been the only drug of oxazolidinone class to reach the market after USFDA approval. Here we review our efforts directed to the discovery of novel oxazolidinone antibacterials evolved through structure-activity relationship (SAR) and an overview of contemporary on going efforts.