(A) Representative examples of biotin-AMP nucleoside-based bisubstrate inhibitors of BPL including: alkylphosphate 10, β-ketophosphonate 11, 1,2,3 triazole 12, acylsulfamate 13, acylsulfamide 14, acylsulfonamide 15, 3-deaza acylsulfamate 16, and 2-tert-butylethynyl-acylsulfamate 17. (B) Benzoxazoline moiety 18, a selective inhibitor of S. aureus BPL. (C) Biotin based inhibitors 19 and 20 of S. aureus BPL.