Synthesis and in vitro antibacterial activities of novel oxazolidinones

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• 作者：Brijesh Kumar Srivastava ; Mukul R. Jain ; Manish Solanki ; Rina Soni ; Darshan Valani ; Sunil Gupta ; Bhupendra Mishra ; Vijay Takale ; Prashant Kapadnis ; Harilal Patel ; Purvi P ; ya ; Jayendra Z. Patel ; Pankaj R. Patel
• 关键词：Piperazinylaryloxazolidinone ; Antibacterial activity ; Linezolid resistant Staphylococcus aureus strain ; In vitro MIC
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：April 2008
• 年：2008
• 卷：43
• 期：4
• 页码：683-693
• 全文大小：618 K

文摘

Design and synthesis of novel piperazinylaryloxazolidinones possessing heteroaryl groups are described and their in vitro antibacterial activities have been evaluated by MIC assay. Compounds (S)-N-[3-{3-fluoro-4-[4-[3-(5-nitrofuran-2-yl)-acryloyl]-piperazin-1-yl]-phenyl}-2-oxo-oxazolidin-5-yl-methyl] acetamide (6o), (S)-N-[3-{3-fluoro-4-[4-[3-(5-nitrothien-2-yl)-acryloyl]-piperazin-1-yl]-phenyl}-2-oxo-oxazolidin-5-yl-methyl] acetamide (6p) and N-oxide of (S)-N-[3-{3-fluoro-4-[4-[3-(5-nitrofuran-2-yl)-acryloyl]-piperazin-1-yl]-phenyl}-2-oxo-oxazolidin-5-yl-methyl] acetamide (9) showed superior antibacterial activities than linezolid and also active against the linezolid resistant Staphylococcus aureus strains.