title: Inhibitors of bacterial tyrosyl tRNA synthetase: synthesis of carbocyclic analogues of the natural product SB-219383.
abstract: Carbocyclic analogues of the microbial metabolite SB-219383 have been synthesised and evaluated as inhibitors of bacterial tyrosyl tRNA synthetase. One compound showed highly potent and selective nanomolar inhibition.
authors.affiliation: GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park, Third Avenue, Harlow, CM19 5AW, Essex, UK.
authors.forename: R L
authors.initials: RL
authors.lastname: Jarvest
authors.forename: J M
authors.initials: JM
authors.lastname: Berge
authors.forename: C S
authors.initials: CS
authors.lastname: Houge-Frydrych
authors.forename: L M
authors.initials: LM
authors.lastname: Mensah
authors.forename: P J
authors.initials: PJ
authors.lastname: O'Hanlon
authors.forename: A J
authors.initials: AJ
authors.lastname: Pope
mesh_terms: D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology; D001671:Biochemistry / Q000379:methods; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000737:chemistry*; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D005663:Furans / Q000737:chemistry*; D013211:Staphylococcus aureus / Q000201:enzymology; D014443:Tyrosine / Q000031:analogs & derivatives* / Q000737:chemistry*; D014448:Tyrosine-tRNA Ligase / Q000037:antagonists & inhibitors*
chemical_list: D000900:Anti-Bacterial Agents; D019086:Bridged Bicyclo Compounds, Heterocyclic; D004791:Enzyme Inhibitors; D005663:Furans; C410784:SB 219383; D014443:Tyrosine; D014448:Tyrosine-tRNA Ligase