Oxazolidinones antibacterials are a novel class of completely chemically synthesized antibacterials with effects of inhibiting multidrug resistant Gram-positive bacteria following sulfonamides and fluoroquinolones.
Linezolid is the first oxazolidinones antibacterial in the market.

Linezolid has relatively strong effects of inhibiting Gram-positive bacteria and does not have cross resistance with other antibacterials. Linezolid has a unique mechanism of action and can inhibit the early phase of the synthesis of bacterioprotein. Linezolid is mainly used for treating infectious diseases induced by resistant Gram-positive bacteria, and can also be used for treating surgical infectious diseases.
CN201010508824.1 discloses TR-701, a pharmaceutical in phase III clinical trial from Trius Therapeutics Inc., which is metabolized in vivo to the active component TR-700, use for infectious diseases induced by Gram-positive bacteria,
However, resistance of Gram-positive bacteria is getting more and more serious clinically. Oxazolidinones antibacterials have a very limited variety of pharmaceuticals for clinical use, currently only linezolid in the market, and cannot meet the clinical needs. In addition, the resistance to linezolid is getting more and more serious. Thus, there is an urgent need to expand varieties of clinically used oxazolidinones antibiotics, and develop antibacterials have highly effective against resistant Gram-positive bacteria.
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