title: New antibacterial tetrahydro-4(2H)-thiopyran and thiomorpholine S-oxide and S,S-dioxide phenyloxazolidinones.
abstract: Combinatorial libraries of N-acylated 5-(S)-aminomethyloxazolidinone derivatives of S-oxide and S,S-dioxide tetrahydro-4(2H)-thiopyranyl and thiomorpholine phenyloxazolidinone series have been synthesized on a solid phase and evaluated for antimicrobial activity. Several novel potent leads have been identified, including orally active oxazolidinones with enhanced activity against respiratory tract infection pathogens Haemophilus influenzae and Moraxella catarrhalis.
authors: Vicuron Pharmaceuticals Inc., 34790 Ardentech Court, Fremont, CA 94555, USA.
authors: Upinder
authors: U
authors: Singh
authors: B
authors: B
authors: Raju
authors: Stuart
authors: S
authors: Lam
authors: Joseph
authors: J
authors: Zhou
authors: Robert C
authors: RC
authors: Gadwood
authors: Charles W
authors: CW
authors: Ford
authors: Gary E
authors: GE
authors: Zurenko
authors: Ronda D
authors: RD
authors: Schaadt
authors: Sara E
authors: SE
authors: Morin
authors: Wade J
authors: WJ
authors: Adams
authors: Janice M
authors: JM
authors: Friis
authors: Maria
authors: M
authors: Courtney
authors: Joe
authors: J
authors: Palandra
authors: Corinne J
authors: CJ
authors: Hackbarth
authors: Sara
authors: S
authors: Lopez
authors: Charlotte
authors: C
authors: Wu
authors: Kathleen H
authors: KH
authors: Mortell
authors: Joaquim
authors: J
authors: Trias
authors: Zhengyu
authors: Z
authors: Yuan
authors: Dinesh V
authors: DV
authors: Patel
authors: Mikhail F
authors: MF
authors: Gordeev
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D001682:Biological Availability; D020650:Combinatorial Chemistry Techniques; D006192:Haemophilus Infections / Q000382:microbiology; D006193:Haemophilus influenzae / Q000187:drug effects*; D050356:Lipid Metabolism; D008297:Male; D008826:Microbial Sensitivity Tests; D001936:Moraxella catarrhalis / Q000187:drug effects*; D045828:Moraxellaceae Infections / Q000382:microbiology; D009025:Morpholines / Q000737:chemistry*; D023303:Oxazolidinones / Q000008:administration & dosage / Q000493:pharmacokinetics*; D010087:Oxides / Q000737:chemistry*; D017601:Oxygen Compounds / Q000493:pharmacokinetics*; D051381:Rats; D017207:Rats, Sprague-Dawley; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D009025:Morpholines; D023303:Oxazolidinones; D010087:Oxides; D017601:Oxygen Compounds; C028971:thiamorpholine