PBTZ169

PBTZ169 is an antibiotic with antimycobacterial activity. It is an irreversible inhibitor of DprE1, an essential enzyme for cell wall synthesis in mycobacteria. PBTZ169 is active against M. tuberculosis in vitro (MIC = ≤0.19 ng/ml) without inducing cytotoxicity in Vero cells when used at concentrations up to 125 μM. It reduces the bacterial burden in the lung and spleen in a mouse model of chronic tuberculosis when administered at a dose of 50 mg/kg per day.

PBTZ169 is a potent irreversible inhibitor of decaprenylphosphoryl-beta-D-ribose 2-epimerase (DprE1), and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro.