Design and synthesis of biaryloxazolidinone derivatives containing amide or acrylamide moiety as novel antibacterial agents against Gram-positive bacteria.
A series of novel biaryloxazolidinone derivatives containing amide and acrylamide structure were designed, synthesized and evaluated for their antibacterial activity. Most compounds generally exhibited potent antibacterial activity with MIC values of 1 μg/mL against S. aureus, MRSA, MSSA, LREF and VRE pathogens, using linezolid and radezolid as positive controls. Compound 17 exhibited good antibacterial activity with MIC values of 0.5 μg/mL against S. aureus, MRSA, MSSA and VRE and 0.25 μg/mL against LREF. The results indicated that compound 17 might serve as a potential hit-compound for further investigation.
['Xu|Sicong|S|', 'Jiang|Jia|J|', 'Qi|Yinliang|Y|', 'Ding|Xiudong|X|', 'Wu|Yachuang|Y|', 'Lei|Hong|H|', 'Zhao|Yanfang|Y|']
D020106:Acrylamide D000577:Amides D000900:Anti-Bacterial Agents D006094:Gram-Positive Bacteria D006801:Humans D015394:Molecular Structure D013329:Structure-Activity Relationship
Biaryloxazolidinone Gram-positive bacteria Antibacterial activity