title: Synthesis and biological evaluation of new N-linked 5-triazolylmethyl oxazolidinones.
abstract: A new series of oxazolidinones bearing N-linked 5-triazolylmethyl group have been synthesized and their in vitro antibacterial activities (MIC) were evaluated against a spectrum of resistant and susceptible Gram-positive organisms. Some of the analogues in this series displayed activity superior to linezolid and vancomycin. Furthermore, in vivo efficacies and pharmacokinetic properties of the selected compounds were also disclosed herein; the selected compounds showed reasonable bioavailability as well as in vivo efficacy comparable to that of linezolid.
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China.
authors.forename: Houxing
authors.initials: H
authors.lastname: Fan
authors.forename: Yilang
authors.initials: Y
authors.lastname: Chen
authors.forename: Zhiteng
authors.initials: Z
authors.lastname: Jiang
authors.forename: Shuhua
authors.initials: S
authors.lastname: Zhang
authors.forename: Dafang
authors.initials: D
authors.lastname: Zhong
authors.forename: Ruyun
authors.initials: R
authors.lastname: Ji
authors.forename: Yushe
authors.initials: Y
authors.lastname: Yang
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001372:Aza Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006094:Gram-Positive Bacteria / Q000187:drug effects / Q000302:isolation & purification; D008745:Methylation; D051379:Mice; D015394:Molecular Structure; D023303:Oxazolidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D001372:Aza Compounds; D023303:Oxazolidinones