title: Synthesis and biological evaluation of novel benzoxazinyl-oxazolidinones as potential antibacterial agents.
abstract: A number of benzoxazinyl-oxazolidinones bearing 3-trizolylmethyl or 3-carboxamide side chain were designed and synthesized with the aim to develop antibacterial agents with improved properties. In vitro antibacterial activities of these novel compounds were evaluated against a panel of resistant and susceptible Gram-positive bacteria. Most analogues bearing 3-trizolylmethyl showed good to moderate antibacterial activities. Compound 12a exhibited a fourfold increase in activity compared with linezolid against all the tested strains, which was identified to be a promising antibacterial agent for further evaluation.
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, Shanghai, China.
authors.forename: Bin
authors.initials: B
authors.lastname: Guo
authors.forename: Houxing
authors.initials: H
authors.lastname: Fan
authors.forename: Qisheng
authors.initials: Q
authors.lastname: Xin
authors.forename: Wenjing
authors.initials: W
authors.lastname: Chu
authors.forename: Hui
authors.initials: H
authors.lastname: Wang
authors.forename: Yushe
authors.initials: Y
authors.lastname: Yang
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D048588:Benzoxazines / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D023303:Oxazolidinones / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D048588:Benzoxazines; D023303:Oxazolidinones