Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones

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).

Graphical abstractDesign and synthesis of a few novel methylamino piperidinyl substituted oxazolidinones are reported and their antibacterial activities have been evaluated in MIC assay against broader panel of both susceptible and resistant Gram-positive strains.Figure optionsDownload full-size imageDownload as PowerPoint slide