Abstract
Oxazolidinones hold great promise as the new line of defense against bacteria that have become resistance to the spectrum of available therapies. Much success has been realized in the treatment of infections by drug resistant Staphylococcus aureus, Enterococcus faecium, and Streptococcus pneumonia strains by the introduction of linezolid (Zyvox). Multidrug resistance involving these pathogens represents one of the largest unmet needs in medicine today. As a class oxazolidinones have not shown great promise in the treatment of gram-negative infections. The overall activity spectrum of this class of drugs is relatively narrow and this has been a significant restriction in their use. The structure activity relationships have been relatively well characterized and the mode of interaction with the ribosome to prevent protein synthesis is being elucidated. The negative effect of linezolid on bone marrow production is a matter of some concern. Several linezolid resistant strains have now been reported.
Keywords: antibacterials; oxazolidinones; linezolid; gram positive; bacteria; ribosome; resistance; synthesis, structure