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Synthesis and biological evaluation of novel benzoxazinyl-oxazolidinones as potential antibacterial agents |
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| Authors: | Bin Guo Houxing Fan Qisheng Xin Wenjing Chu Hui Wang Yushe Yang |
| Institution: | 1. State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, Shanghai, China;2. Department of Microbiology, China Pharmaceutical University, Nanjing, Jiangsu Province 210009, China |
| Abstract: | A number of benzoxazinyl-oxazolidinones bearing 3-trizolylmethyl or 3-carboxamide side chain were designed and synthesized with the aim to develop antibacterial agents with improved properties. In vitro antibacterial activities of these novel compounds were evaluated against a panel of resistant and susceptible Gram-positive bacteria. Most analogues bearing 3-trizolylmethyl showed good to moderate antibacterial activities. Compound 12a exhibited a fourfold increase in activity compared with linezolid against all the tested strains, which was identified to be a promising antibacterial agent for further evaluation. |
| Keywords: | Benzoxazinyl-oxazolidinone Linezolid Antibacterial agents Gram-positive organisms |
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