PBTZ169 是具有杀菌作用的苯并噻嗪酮，也有抗结核作用。它也是一种DprE1有效抑制剂，可通过与活性位点 Cys387 残基形成共价键来抑制必需的黄素蛋白 DprE1。

PBTZ169 inhibits decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1), more efficiently than BTZ043.

PBTZ169, inhibit decaprenylphosphoryl-β-d-ribose 2′-oxidase (DprE1) and display nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro.

PBTZ169 can be suspend in 0.25% hydroxy-propylmethyl-cellulose. The administertration for PBTZ169 is 100 mg/kg by gavage. The MIC50 and MIC90 values were 0.0075 and 0.030 μg/mL, respectively. The MIC for PBTZ169 for N. brasiliensis HUJEG-1 was 0.0037 μg/mL. PBTZ169 has improved potency, safety and efficacy in zebrafish and mouse models of tuberculosis (TB).

1377239-83-2

C20H23F3N4O3S

456.48

PBTZ169

DMSO:6.4 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years