title: New Series of BPL Inhibitors To Probe the Ribose-Binding Pocket ofStaphylococcus aureusBiotin Protein Ligase.
abstract: Replacing the labile adenosinyl-substituted phosphoanhydride of biotinyl-5'-AMP with a N1-benzyl substituted 1,2,3-triazole gave a new truncated series of inhibitors ofStaphylococcus aureusbiotin protein ligase (SaBPL). The benzyl group presents to the ribose-binding pocket ofSaBPL based onin silicodocking. Halogenated benzyl derivatives (12t,12u,12w, and12x) proved to be the most potent inhibitors ofSaBPL. These derivatives inhibited the growth ofS. aureusATCC49775 and displayed low cytotoxicity against HepG2 cells.
authors.affiliation: Department of Chemistry, Department of Molecular and Cellular Biology, and Centre for Nanoscale BioPhotonics (CNBP), University of Adelaide , Adelaide, South Australia 5005, Australia.
authors.forename: Jiage
authors.initials: J
authors.lastname: Feng
authors.affiliation: Department of Chemistry, Department of Molecular and Cellular Biology, and Centre for Nanoscale BioPhotonics (CNBP), University of Adelaide , Adelaide, South Australia 5005, Australia.
authors.forename: Ashleigh S
authors.initials: AS
authors.lastname: Paparella
authors.affiliation: Department of Chemistry, Department of Molecular and Cellular Biology, and Centre for Nanoscale BioPhotonics (CNBP), University of Adelaide , Adelaide, South Australia 5005, Australia.
authors.forename: William
authors.initials: W
authors.lastname: Tieu
authors.affiliation: Department of Chemistry, Department of Molecular and Cellular Biology, and Centre for Nanoscale BioPhotonics (CNBP), University of Adelaide , Adelaide, South Australia 5005, Australia.
authors.forename: David
authors.initials: D
authors.lastname: Heim
authors.affiliation: Department of Chemistry, Department of Molecular and Cellular Biology, and Centre for Nanoscale BioPhotonics (CNBP), University of Adelaide , Adelaide, South Australia 5005, Australia.
authors.forename: Sarah
authors.initials: S
authors.lastname: Clark
authors.affiliation: Department of Chemistry, Department of Molecular and Cellular Biology, and Centre for Nanoscale BioPhotonics (CNBP), University of Adelaide , Adelaide, South Australia 5005, Australia.
authors.forename: Andrew
authors.initials: A
authors.lastname: Hayes
authors.affiliation: Department of Chemistry, Department of Molecular and Cellular Biology, and Centre for Nanoscale BioPhotonics (CNBP), University of Adelaide , Adelaide, South Australia 5005, Australia.
authors.forename: Grant W
authors.initials: GW
authors.lastname: Booker
authors.affiliation: Department of Chemistry, Department of Molecular and Cellular Biology, and Centre for Nanoscale BioPhotonics (CNBP), University of Adelaide , Adelaide, South Australia 5005, Australia.
authors.forename: Steven W
authors.initials: SW
authors.lastname: Polyak
authors.affiliation: Department of Chemistry, Department of Molecular and Cellular Biology, and Centre for Nanoscale BioPhotonics (CNBP), University of Adelaide , Adelaide, South Australia 5005, Australia.
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Abell
keywords: Enzyme inhibitors; Staphylococcus aureus; antibiotics; biotin protein ligase