title: Biaryl isoxazolinone antibacterial agents.
abstract: In an era of increasing resistance to classical antibacterial agents, the synthetic oxazolidinone series of antibiotics has attracted much interest. Zyvoxtrade mark was the first oxazolidinone to be approved for clinical use against infections caused by multi-drug resistant Gram-positive bacteria. In the course of studies directed toward the discovery of novel antibacterial agents, a new series of synthetic phenyl-isoxazolinone agents that displayed potent activity against Gram-positive bacterial strains was recently discovered at Bristol-Myers Squibb. Extensive investigation of various substitutions on the phenyl ring was then undertaken. We report here, the synthesis and antibacterial activity of a series of biaryl isoxazolinone compounds.
authors.affiliation: Bristol-Myers Squibb Pharmaceutical Research Institute, Discovery Chemistry, Candiac, Québec, Canada. claude.quesnelle@hms.com
authors.forename: Claude A
authors.initials: CA
authors.lastname: Quesnelle
authors.forename: Patrice
authors.initials: P
authors.lastname: Gill
authors.forename: Stephan
authors.initials: S
authors.lastname: Roy
authors.forename: Marco
authors.initials: M
authors.lastname: Dodier
authors.forename: Anne
authors.initials: A
authors.lastname: Marinier
authors.forename: Alain
authors.initials: A
authors.lastname: Martel
authors.forename: Lawrence B
authors.initials: LB
authors.lastname: Snyder
authors.forename: Stanley V
authors.initials: SV
authors.lastname: D'Andrea
authors.forename: Joanne J
authors.initials: JJ
authors.lastname: Bronson
authors.forename: Marybeth
authors.initials: M
authors.lastname: Frosco
authors.forename: Danielle
authors.initials: D
authors.lastname: Beaulieu
authors.forename: Glen A
authors.initials: GA
authors.lastname: Warr
authors.forename: Ken L
authors.initials: KL
authors.lastname: Denbleyker
authors.forename: Terry M
authors.initials: TM
authors.lastname: Stickle
authors.forename: Hyekyung
authors.initials: H
authors.lastname: Yang
authors.forename: Susan E
authors.initials: SE
authors.lastname: Chaniewski
authors.forename: Cheryl A
authors.initials: CA
authors.lastname: Ferraro
authors.forename: Dennis
authors.initials: D
authors.lastname: Taylor
authors.forename: John W
authors.initials: JW
authors.lastname: Russell
authors.forename: Kenneth S
authors.initials: KS
authors.lastname: Santone
authors.forename: Junius
authors.initials: J
authors.lastname: Clarke
authors.forename: Rebecca L
authors.initials: RL
authors.lastname: Drain
authors.forename: Jay O
authors.initials: JO
authors.lastname: Knipe
authors.forename: Kathleen
authors.initials: K
authors.lastname: Mosure
authors.forename: John F
authors.initials: JF
authors.lastname: Barrett
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D006193:Haemophilus influenzae / Q000187:drug effects; D007555:Isoxazoles / Q000737:chemistry* / Q000494:pharmacology*; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D007555:Isoxazoles