The synthesis and antimicrobial evaluation of a new series of isoxazolinyl oxazolidinones.
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.
Weidner-Wells
Michele A
MA
Antimicrobial Agents Research Team, Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, LL C, 1000 Route 202, Raritan, NJ 08869, USA.
Werblood
Harvey M
HM
Goldschmidt
Raul
R
Bush
Karen
K
Foleno
Barbara D
BD
Hilliard
Jamese J
JJ
Melton
John
J
Wira
Ellyn
E
Macielag
Mark J
MJ
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
D000900:Anti-Bacterial Agents; D007555:Isoxazoles; D023303:Oxazolidinones