Design, synthesis, and antibacterial evaluation of a novel series of biaryloxazolidinone derivatives against Gram-positive bacteria

A series of new biaryloxazolidinone derivatives has been designed and synthesized using the combination principle and blocking metabolic site to improve their antibacterial activity and stability. Apart from the excellent antibacterial profile against S. aureus (MIC = 0.25 mu g mL(-1)), MRSA (MIC = 0.25 mu g mL(-1)), LREF (MIC = 0.031 mu g mL(-1)), VRE (MIC = 0.031 mu g mL(-1)), GBS (MIC = 0.031 mu g mL(-1)), and Spn (MIC = 0.031 mu g mL(-1)), compound 13b-6 also displayed good stability and safety, excellent rat PK profile with long half-life time (T-1/2 = 17.7 h), and moderate plasma exposure (AUC(0-t) = 74.4 ng mL(-1)).