Biaryl isoxazolinone antibacterial agents.
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.
Quesnelle
Claude A
CA
Bristol-Myers Squibb Pharmaceutical Research Institute, Discovery Chemistry, Candiac, Québec, Canada. claude.quesnelle@hms.com
Gill
Patrice
P
Roy
Stephan
S
Dodier
Marco
M
Marinier
Anne
A
Martel
Alain
A
Snyder
Lawrence B
LB
D'Andrea
Stanley V
SV
Bronson
Joanne J
JJ
Frosco
Marybeth
M
Beaulieu
Danielle
D
Warr
Glen A
GA
Denbleyker
Ken L
KL
Stickle
Terry M
TM
Yang
Hyekyung
H
Chaniewski
Susan E
SE
Ferraro
Cheryl A
CA
Taylor
Dennis
D
Russell
John W
JW
Santone
Kenneth S
KS
Clarke
Junius
J
Drain
Rebecca L
RL
Knipe
Jay O
JO
Mosure
Kathleen
K
Barrett
John F
JF
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
D000900:Anti-Bacterial Agents; D007555:Isoxazoles