Oxazolidinones are mainly used as antimicrobials. The antibacterial effect of oxazolidinones is by working as protein synthesis inhibitors, targeting an early step involving the binding of N-formylmethionyl-tRNA to the ribosome.

Oxazolidinones have shown activity against M.tb and several are either in development for, or already used to treat TB. Linezolid, Sutezolid, and Cycloserine are all members of the oxazolidinone class.