title: Synthesis and in vitro antibacterial activities of novel oxazolidinones.
abstract: 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.
authors.affiliation: Zydus Research Centre, Department of Medicinal Chemistry, Sarkhej-Bavla N.H.8A, Moraiya, Ahmedabad 382210, Gujarat, India. brijeshsrivastava@zyduscadila.com
authors.forename: Brijesh Kumar
authors.initials: BK
authors.lastname: Srivastava
authors.forename: Mukul R
authors.initials: MR
authors.lastname: Jain
authors.forename: Manish
authors.initials: M
authors.lastname: Solanki
authors.forename: Rina
authors.initials: R
authors.lastname: Soni
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: Prashant
authors.initials: P
authors.lastname: Kapadnis
authors.forename: Harilal
authors.initials: H
authors.lastname: Patel
authors.forename: Purvi
authors.initials: P
authors.lastname: Pandya
authors.forename: Jayendra Z
authors.initials: JZ
authors.lastname: Patel
authors.forename: Pankaj R
authors.initials: PR
authors.lastname: Patel
mesh_terms: D000081:Acetamides / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D015195:Drug Design; D000069349:Linezolid; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: D000081:Acetamides; D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D000069349:Linezolid