Novel piperidinyloxy oxazolidinone antimicrobial agents.
Oxazolidinone antibacterial agents, where the N-substituted piperazinyl group of eperezolid was replaced with a N-substituted piperidinyloxy moiety, were synthesized and shown to be active against a variety of resistant and susceptible Gram-positive organisms. The effect of ring size, positional isomerism, and fluorine substitution on antibacterial activity was examined.
Weidner-Wells
M A
MA
Drug Discovery, The R. W. Johnson Pharmaceutical Research Institute, 1000 Route 202, 08869, Raritan, NJ, USA. mwells@prius.jnj.com
Boggs
C M
CM
Foleno
B D
BD
Wira
E
E
Bush
K
K
Goldschmidt
R M
RM
Hlasta
D J
DJ
D000081:Acetamides / Q000737:chemistry; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D004351:Drug Resistance / Q000502:physiology; D004926:Escherichia coli / Q000187:drug effects*; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D010080:Oxazoles / Q000737:chemistry; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000494:pharmacology*; D010880:Piperidines / Q000737:chemistry; D013211:Staphylococcus aureus / Q000187:drug effects*
D000081:Acetamides; D000900:Anti-Bacterial Agents; D010080:Oxazoles; D023303:Oxazolidinones; D010880:Piperidines; C098011:eperezolid