Recent developments in the discovery of novel oxazolidinone antibacterials.

The oxazolidinone antibacterials represent an unusual example of a new synthetic class of compounds for the treatment of drug-resistant Gram-positive infections. The first clinically approved example of this class is linezolid, which, despite showing considerable clinical promise, can cause side effects that prevent general use of the drug in the community. New research has been directed toward broadening the antibacterial spectrum of this class of compound, re-establishing sensitivity to linezolid-resistant strains and lowering the toxicity potential. This research has yielded new bioisosteres of the oxazolidinone ring and, in another approach, created hybrid structures with existing Gram-negative active drug classes. New oxazolidinone-based drugs are in early clinical development and indications are that this class of antibacterials will continue to show promise.