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Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones
Authors:Srivastava Brijesh Kumar  Soni Rina  Patel Jayendra Z  Solanki Manish  Valani Darshan  Gupta Sunil  Mishra Bhupendra  Takale Vijay  Pandya Purvi  Jain Mukul R  Patel Pankaj R
Affiliation:Zydus Research Centre, Sarkhej-Bavla N. H.8A, Moraiya, Ahmedabad 382210, India. brijeshsrivastava@zyduscadila.com
Abstract: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 microg/mL against linezolid resistant Staphylococcus aureus (linezolid 16 microg/mL).
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