title: Structure-activity relationships of the peptide deformylase inhibitor BB-3497: modification of the metal binding group.
abstract: A series of analogues of the potent peptide deformylase (PDF) inhibitor BB-3497 containing alternative metal binding groups was synthesised. Enzyme inhibition and antibacterial activity data for these compounds revealed that the bidentate hydroxamic acid and N-formyl hydroxylamine structural motifs represent the optimum chelating groups on the pseudopeptidic BB-3497 backbone.
authors.affiliation: British Biotech Pharmaceuticals Limited, Watlington Road, Oxford OX4 6LY, UK.
authors.forename: Helen K
authors.initials: HK
authors.lastname: Smith
authors.forename: R Paul
authors.initials: RP
authors.lastname: Beckett
authors.forename: John M
authors.initials: JM
authors.lastname: Clements
authors.forename: Sheila
authors.initials: S
authors.lastname: Doel
authors.forename: Stephen P
authors.initials: SP
authors.lastname: East
authors.forename: Steven B
authors.initials: SB
authors.lastname: Launchbury
authors.forename: Lisa M
authors.initials: LM
authors.lastname: Pratt
authors.forename: Zoë M
authors.initials: ZM
authors.lastname: Spavold
authors.forename: Wayne
authors.initials: W
authors.lastname: Thomas
authors.forename: Richard S
authors.initials: RS
authors.lastname: Todd
authors.forename: Mark
authors.initials: M
authors.lastname: Whittaker
mesh_terms: D000581:Amidohydrolases; D000626:Aminopeptidases / Q000037:antagonists & inhibitors*; D001419:Bacteria / Q000187:drug effects; D001665:Binding Sites; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D029968:Escherichia coli Proteins / Q000037:antagonists & inhibitors; D006877:Hydroxamic Acids / Q000138:chemical synthesis* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D008670:Metals / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
chemical_list: C425109:BB3497; D004791:Enzyme Inhibitors; D029968:Escherichia coli Proteins; D006877:Hydroxamic Acids; D008670:Metals; D000626:Aminopeptidases; D000581:Amidohydrolases; C084507:peptide deformylase