title: Synthesis and antibacterial activity of oxazolidinones containing pyridine substituted with heteroaromatic ring.
abstract: A series of oxazolidinone derivatives, which morpholino group of linezolid was replaced with heteroaromatic ring substituted pyridine moiety, were newly synthesized, and their substituted effects on in vitro and in vivo antibacterial activities were evaluated against four problematic gram-positive strains including drug resistant strains and two gram-negative strains. Most compounds exhibited the enhanced in vitro activities with 4-16-fold and three compounds exerted more than 2-fold increased in vivo efficacies than linezolid.
authors.affiliation: College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul 151-742, Korea.
authors.forename: Yeong Woo
authors.initials: YW
authors.lastname: Jo
authors.forename: Weon Bin
authors.initials: WB
authors.lastname: Im
authors.forename: Jae Keol
authors.initials: JK
authors.lastname: Rhee
authors.forename: Mi Ja
authors.initials: MJ
authors.lastname: Shim
authors.forename: Won Bae
authors.initials: WB
authors.lastname: Kim
authors.forename: Eung Chil
authors.initials: EC
authors.lastname: Choi
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D023303:Oxazolidinones; D011725:Pyridines; C023666:pyridine