Heterocyclic acyl-phosphate bioisostere-based inhibitors of Staphylococcus aureus biotin protein ligase Academic Article uri icon


  • Inhibitors of Staphylococcus aureus biotin protein ligase (SaBPL) are generated by replacing the acyl phosphate group of biotinyl-5'-AMP with either a 1,2,3-triazole (see 5/10a/10b) or a 1,2,4-oxadiazole (see 7) bioisostere. Importantly, the inhibitors are inactive against the human BPL. The nature of the 5-substituent in the component benzoxazolone of the optimum 1,2,3-triazole series is critical to activity, where this group binds in the ATP binding pocket of the enzyme.


  • Tieu, W
  • Jarrad, AM
  • Paparella, AS
  • Keeling, KA
  • Soares Da Costa, TP
  • Wallace, JC
  • Booker, GW
  • Polyak, SW
  • Abell, AD

publication date

  • 2014