Oxazolidinones: a novel class of antibiotics

Abstract.

Oxazolidinones are a novel class of synthetic antimicrobial agents which have now entered phase III clinical trials. The most promising feature of these compounds is their oral activity against multidrug-resistant Gram-positive bacteria which have created tremendous therapeutic problems in recent years. In addition, development of resistance in vitro has so far remained below detectable levels. Different from many antibacterial agents used in the treatment of human infections, oxazolidinones do not block bacterial protein synthesis at the level of polypeptide chain elongation but rather seem to interfere with initiation of translation. Both binding of formylmethionine-transfer RNA to initiation complexes as well as release of formylmethionine-puromycin from initiation complexes have been reported to be targets for oxazolidinones. The major binding sites of oxazolidinones are the large (50S) ribosomal subunits.