摘要：

Since the introduction in the pharmaceutical market of linezolid, an oxazolidin-2-one based new class of antibacterial agents with a unique mechanism of action, this cyclic carbamate bought a wider popularity and interest for the scientific community. In fact the 1,3-oxazolidin-2-one nucleus is a popular heterocycle framework in synthetic organic chemistry for its use as chiral auxiliary in stereoselective transformations. This chapter describes the antibacterial activity of linezolid and the status of the activities of other oxazolidin-2-ones based antibacterial agents under active clinical investigation. Linezolid and other oxazolidin-2-one antibacterial agents are currently prepared by chemical synthesis via diverse synthetic routes that have been extensively studied in academic and industrial labs. Biological active oxazolidin-2-one derivatives are quite rare among natural products.

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