Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones
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- 作者：Brijesh Kumar Srivastava ; Rina Soni ; Jayendra Z. Patel ; Manish Solanki ; Darshan Valani ; Sunil Gupta ; Bhupendra Mishra ; Vijay Takale ; Purvi P ; ya ; Mukul R. Jain ; Pankaj R. Patel
- 关键词：N-Methylamino piperidinylaryloxazolidinones ; In vitro MIC assay ; Gram-positive organism ; Linezolid resistant Staphylococcus aureus
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 出版时间：15 September 2007
- 年：2007
- 卷：17
- 期：18
- 页码：5227-5232
- 全文大小：157 K
文摘
Design and synthesis of a few novel methylamino piperidinyl substituted oxazolidinones are reported. Their antibacterial activities have been evaluated in a MIC assay against broader panel of both susceptible and resistant Gram-positive strains. (S)-N-{3-[3-Fluoro-4-(methyl-{1-[3-(5-nitrofuran-2-yl)-acryloyl]-piperidin-4-yl}-amino)-phenyl]-2-oxo-oxazolidin-5-ylmethyl}-acetamide 4i has shown comparable antibacterial activity to linezolid and eperezolid in the MIC assay, additionally compound 4i showed good antibacterial activity with an in vitro MIC value of 2–4 μg/mL against linezolid resistant Staphylococcus aureus (linezolid ![]()
16 μg/mL).