Synthesis and SAR of novel conformationally restricted oxazolidinones possessing gram-positive and fastidious gram-negative antibacterial activity. Part 2: Amino substitutions on heterocyclic D-ring system.
A novel series of conformationally restricted oxazolidinones was synthesized, in which the heterocyclic D ring was substituted with various amino groups. Several analogs exhibited potent activity against both gram-positive and fastidious gram-negative organisms. Certain amino-substituted analogs also exhibited improved aqueous solubility compared to the corresponding un-substituted heterocyclic D-ring analogs.
Choy
Allison L
AL
Pfizer Global Research and Development, 2800 Plymouth Rd., Ann Arbor, MI 48105, USA. Allison.Choy@pfizer.com
Vara Prasad
J V N
JV
Boyer
Frederick E
FE
Huband
Michael D
MD
Dermyer
Michael R
MR
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D015394:Molecular Structure; D023303:Oxazolidinones / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D023303:Oxazolidinones