title: 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.
abstract: 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.
authors.affiliation: Pfizer Global Research and Development, 2800 Plymouth Rd., Ann Arbor, MI 48105, USA. Allison.Choy@pfizer.com
authors.forename: Allison L
authors.initials: AL
authors.lastname: Choy
authors.forename: J V N
authors.initials: JV
authors.lastname: Vara Prasad
authors.forename: Frederick E
authors.initials: FE
authors.lastname: Boyer
authors.forename: Michael D
authors.initials: MD
authors.lastname: Huband
authors.forename: Michael R
authors.initials: MR
authors.lastname: Dermyer
mesh_terms: 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
chemical_list: D000900:Anti-Bacterial Agents; D023303:Oxazolidinones