title: Synthesis and in vitro antibacterial activity of novel methylamino piperidinyl oxazolidinones.
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).
authors.affiliation: Zydus Research Centre, Sarkhej-Bavla N. H.8A, Moraiya, Ahmedabad 382210, India. brijeshsrivastava@zyduscadila.com
authors.forename: Brijesh Kumar
authors.initials: BK
authors.lastname: Srivastava
authors.forename: Rina
authors.initials: R
authors.lastname: Soni
authors.forename: Jayendra Z
authors.initials: JZ
authors.lastname: Patel
authors.forename: Manish
authors.initials: M
authors.lastname: Solanki
authors.forename: Darshan
authors.initials: D
authors.lastname: Valani
authors.forename: Sunil
authors.initials: S
authors.lastname: Gupta
authors.forename: Bhupendra
authors.initials: B
authors.lastname: Mishra
authors.forename: Vijay
authors.initials: V
authors.lastname: Takale
authors.forename: Purvi
authors.initials: P
authors.lastname: Pandya
authors.forename: Mukul R
authors.initials: MR
authors.lastname: Jain
authors.forename: Pankaj R
authors.initials: PR
authors.lastname: Patel
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010880:Piperidines / Q000737:chemistry*
chemical_list: D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D010880:Piperidines