Design, synthesis, and antibacterial evaluation of a novel series of biaryloxazolidinone derivatives against Gram-positive bacteria?
New Journal of Chemistry Pub Date: 2022-04-18 DOI: 10.1039/D2NJ00479H
Abstract
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 μg mL?1), MRSA (MIC = 0.25 μg mL?1), LREF (MIC = 0.031 μg mL?1), VRE (MIC = 0.031 μg mL?1), GBS (MIC = 0.031 μg mL?1), and Spn (MIC = 0.031 μg mL?1), compound 13b-6 also displayed good stability and safety, excellent rat PK profile with long half-life time (T1/2 = 17.7 h), and moderate plasma exposure (AUC0–t = 74.4 ng mL?1).
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Journal Name：New Journal of Chemistry
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CAS no.: 89640-58-4
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