BPH-1358

BPH-1358 is an inhibitor of undecaprenyl diphosphate synthase (UPPS; IC₅₀ = 0.11 µM for the E. coli and S. aureus enzymes), an enzyme involved in bacterial cell wall biosynthesis.¹ It is also an inhibitor of farnesyl diphosphate synthase (FPPS; IC₅₀ = 1.8 µM for the human enzyme), an enzyme in the mevalonate pathway of cholesterol and isoprenoid biosynthesis.² BPH-1358 is active against E. coli and S. aureus (EC₅₀s = 0.3 and 0.29 nM, respectively) and increases survival in a mouse model of S. aureus infection when administered at a dose of 10 mg/kg.¹

1.Zhu, W., Wang, Y., Li, K., et al.Antibacterial drug leads: DNA and enzyme multitargetingJ. Med. Chem.58(3)1215-1227(2015) 2.Lindert, S., Zhu, W., Liu, Y.-L., et al.Farnesyl diphosphate synthase inhibitors from in silico screeningChem. Biol. Drug Des.81(6)742-748(2013)