title: In vitro and intracellular activities of peptide deformylase inhibitor GSK1322322 against Legionella pneumophila isolates.
abstract: GSK1322322, a novel peptide deformylase inhibitor currently in development as an oral and intravenous agent for the treatment of hospitalized community-acquired bacterial pneumonia, showed poor in vitro activity against a panel of 50 Legionella pneumophila strains, with MICs ranging from 1 to 16 μg/ml and an MIC90 of 16 μg/ml, but very potent intracellular activity, with the minimum extracellular concentrations capable of inhibiting intracellular proliferation (MIECs) ranging from 0.12 to 2 μg/ml and 98% of the strains being inhibited by concentrations of ≤ 1 μg/ml.
authors.affiliation: M360, Sherbrooke, Québec, Canada.
authors.forename: Jacques
authors.initials: J
authors.lastname: Dubois
authors.affiliation: M360, Sherbrooke, Québec, Canada.
authors.forename: Maïtée
authors.initials: M
authors.lastname: Dubois
authors.affiliation: M360, Sherbrooke, Québec, Canada.
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Martel
authors.affiliation: Antibacterial Discovery Performance Unit, Infectious Disease Therapeutic Area, GlaxoSmithKline, Collegeville, Pennsylvania, USA.
authors.forename: Kelly
authors.initials: K
authors.lastname: Aubart
authors.affiliation: Antibacterial Discovery Performance Unit, Infectious Disease Therapeutic Area, GlaxoSmithKline, Collegeville, Pennsylvania, USA deborah.l.butler@gsk.com.
authors.forename: Deborah
authors.initials: D
authors.lastname: Butler
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology* / Q000627:therapeutic use; D017963:Azithromycin / Q000494:pharmacology; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D006877:Hydroxamic Acids / Q000494:pharmacology* / Q000627:therapeutic use; D016952:Legionella pneumophila / Q000187:drug effects*; D007877:Legionnaires' Disease / Q000188:drug therapy; D064704:Levofloxacin / Q000494:pharmacology; D008826:Microbial Sensitivity Tests
chemical_list: D000900:Anti-Bacterial Agents; D019086:Bridged Bicyclo Compounds, Heterocyclic; C583947:GSK1322322; D006877:Hydroxamic Acids; D064704:Levofloxacin; D017963:Azithromycin