Design and synthesis of biaryloxazolidinone derivatives containing amide or acrylamide moiety as novel antibacterial agents against Gram-positive bacteria |
| |
Affiliation: | 1. Research Promotion, Ono Pharmaceutical Co., Ltd., Shimamoto, Osaka 618-8585, Japan;2. Discovery Research Laboratories, Ono Pharmaceutical Co., Ltd., Shimamoto, Osaka 618-8585, Japan;3. Department of Orthopedic Surgery, Kagawa University Faculty of Medicine, Mikicho, Kagawa 761-0793, Japan |
| |
Abstract: | 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. |
| |
Keywords: | Biaryloxazolidinone Antibacterial activity Gram-positive bacteria |
本文献已被 ScienceDirect 等数据库收录! |
|