title: Synthesis and antibacterial activity of [6,5,5] and [6,6,5] tricyclic fused oxazolidinones.
abstract: A series of conformationally restricted, [6,5,5] and [6,6,5] tricyclic fused oxazolidinones were synthesized and tested for antibacterial activity. Several compounds in the trans-[6,5,5] series demonstrated potent in vitro and in vivo activity. This work provides valuable information regarding the preferred conformational orientation of the oxazolidinones at the binding site.
authors.affiliation: Pharmacia & Upjohn, Kalamazoo, MI 49001, USA.
authors.forename: D M
authors.initials: DM
authors.lastname: Gleave
authors.forename: S J
authors.initials: SJ
authors.lastname: Brickner
authors.forename: P R
authors.initials: PR
authors.lastname: Manninen
authors.forename: D A
authors.initials: DA
authors.lastname: Allwine
authors.forename: K D
authors.initials: KD
authors.lastname: Lovasz
authors.forename: D C
authors.initials: DC
authors.lastname: Rohrer
authors.forename: J A
authors.initials: JA
authors.lastname: Tucker
authors.forename: G E
authors.initials: GE
authors.lastname: Zurenko
authors.forename: C W
authors.initials: CW
authors.lastname: Ford
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D001424:Bacterial Infections / Q000188:drug therapy*; D007202:Indicators and Reagents; D051379:Mice; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D008968:Molecular Conformation; D015394:Molecular Structure; D010080:Oxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D007202:Indicators and Reagents; D010080:Oxazoles