title: Peptide deformylase inhibitors with activity against respiratory tract pathogens.
abstract: A series of analogues of the peptide deformylase (PDF) inhibitor BB-3497 where the P3' amide bond was replaced with a ketone functionality is described. The in vitro antibacterial profiling of these compounds revealed that they demonstrate activity against pathogens associated with respiratory tract infections.
authors.affiliation: British Biotech Pharmaceuticals Limited, Watlington Road, Oxford OX4 6LY, UK. stephen.east@evotecoai.com
authors.forename: Stephen P
authors.initials: SP
authors.lastname: East
authors.forename: R Paul
authors.initials: RP
authors.lastname: Beckett
authors.forename: Daniel C
authors.initials: DC
authors.lastname: Brookings
authors.forename: John M
authors.initials: JM
authors.lastname: Clements
authors.forename: Sheila
authors.initials: S
authors.lastname: Doel
authors.forename: Kenneth
authors.initials: K
authors.lastname: Keavey
authors.forename: Gilles
authors.initials: G
authors.lastname: Pain
authors.forename: Helen K
authors.initials: HK
authors.lastname: Smith
authors.forename: Wayne
authors.initials: W
authors.lastname: Thomas
authors.forename: Alison J
authors.initials: AJ
authors.lastname: Thompson
authors.forename: Richard S
authors.initials: RS
authors.lastname: Todd
authors.forename: Mark
authors.initials: M
authors.lastname: Whittaker
mesh_terms: D000581:Amidohydrolases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D000890:Anti-Infective Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D006193:Haemophilus influenzae / Q000187:drug effects / Q000201:enzymology; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D001936:Moraxella catarrhalis / Q000187:drug effects / Q000201:enzymology; D012141:Respiratory Tract Infections / Q000201:enzymology* / Q000382:microbiology*; D013296:Streptococcus pneumoniae / Q000187:drug effects / Q000201:enzymology
chemical_list: D000890:Anti-Infective Agents; D004791:Enzyme Inhibitors; D000581:Amidohydrolases; C084507:peptide deformylase