title: Synthesis and antibacterial activity of arylpiperazinyl oxazolidinones with diversification of the N-substituents.
abstract: A series of 4-arylpiperazin-1-yl-3-phenyloxazolidin-2-one derivatives with diversification of the N-substituents such as methylene O-linked heterocycles, thioamide, dithiocarbamate, thiourea, and thiocarbamate were synthesized and evaluated as antibacterial agents. Their in vitro activities (MIC) were evaluated against MRSA and VRE resistant Gram-positive strains such as Staphylococcus and Enterococcus. Most of the compounds were more potent in vitro but less active in vivo than linezolid.
authors.affiliation: Imagene Co. Ltd, Biotechnology Incubating Center, Seoul National University, Seoul 151-742, South Korea.
authors.forename: Sun-Young
authors.initials: SY
authors.lastname: Jang
authors.forename: Young Hwan
authors.initials: YH
authors.lastname: Ha
authors.forename: Seung Whan
authors.initials: SW
authors.lastname: Ko
authors.forename: Wonku
authors.initials: W
authors.lastname: Lee
authors.forename: Jongkook
authors.initials: J
authors.lastname: Lee
authors.forename: Sunghoon
authors.initials: S
authors.lastname: Kim
authors.forename: Yong Woo
authors.initials: YW
authors.lastname: Kim
authors.forename: Won Koo
authors.initials: WK
authors.lastname: Lee
authors.forename: Hyun-Joon
authors.initials: HJ
authors.lastname: Ha
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D013293:Enterococcus faecalis / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D008968:Molecular Conformation; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013210:Staphylococcus / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D010879:Piperazines