Synthesis and structure-activity studies of novel homomorpholine oxazolidinone antibacterial agents.
A novel series of oxazolidinones were synthesized in which the morpholine C-ring of linezolid was replaced with homomorpholine. In addition to investigating the effect of a homomorpholine C-ring on antibacterial activity, the effect of des-, mono-, di-, and tri-fluoro substitution on the phenyl B-ring was investigated as well. Various C-5 functional groups were also examined, including acetamides and triazoles and carboxamides.
Kim
Ji-Young
JY
Pfizer Global Research and Development, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. ji-young.kim@pfizer.com
Boyer
Frederick E
FE
Choy
Allison L
AL
Huband
Michael D
MD
Pagano
Paul J
PJ
Vara Prasad
J V N
JV
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D009025:Morpholines / Q000737:chemistry*; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D009025:Morpholines; D023303:Oxazolidinones; C037574:morpholine