title: The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones.
abstract: A series of oxazolidinone antibacterial agents containing a 5-substituted isoxazol-3-yl moiety were synthesized via a nitrile oxide [3+2] dipolar cycloaddition reaction. These compounds were screened against a panel of susceptible and resistant Gram-positive organisms. Several analogs from this series were comparable to or more potent than linezolid in vitro.
authors.affiliation: Antimicrobial Agents Research Team, Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, LL C, 1000 Route 202, Raritan, NJ 08869, USA.
authors.forename: Michele A
authors.initials: MA
authors.lastname: Weidner-Wells
authors.forename: Harvey M
authors.initials: HM
authors.lastname: Werblood
authors.forename: Raul
authors.initials: R
authors.lastname: Goldschmidt
authors.forename: Karen
authors.initials: K
authors.lastname: Bush
authors.forename: Barbara D
authors.initials: BD
authors.lastname: Foleno
authors.forename: Jamese J
authors.initials: JJ
authors.lastname: Hilliard
authors.forename: John
authors.initials: J
authors.lastname: Melton
authors.forename: Ellyn
authors.initials: E
authors.lastname: Wira
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Macielag
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D004353:Drug Evaluation, Preclinical / Q000379:methods; D005260:Female; D007555:Isoxazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D051379:Mice; D008826:Microbial Sensitivity Tests / Q000379:methods; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D007555:Isoxazoles; D023303:Oxazolidinones