Abstract
The oxazolidinone class of antibacterial agents, as exemplified by linezolid (Zyvox®, Pharmacia Corp.), represents the first completely new class of antibacterial agents to achieve regulatory approval in over 30 years. Due to their potent activity against multi-drug resistant Gram-positive bacteria, discovery research in this area has flourished, with many pharmaceutical companies worldwide beginning research programmes. With the expanded research efforts, new understanding of the oxazolidinone structure–activity relationship has led to an increased spectrum of activity to include the fastidious Gram-negative pathogens Haemophilus influenzae and Moraxella catarrhalis. In addition, a deeper understanding of the toxicology, mechanism of action, and mechanism of resistance has emerged.