BTZ043 是一种 DprE1 的抑制剂，它对结核分枝杆菌 H37Rv 和耻垢分枝杆菌具有纳摩尔杀菌活性，MIC 值分别为 2.3 nM 和 9.2 nM。

BTZ043 is a DprE1 inhibitor with nanomolar bactericidal activity against Mycobacterium tuberculosis in vitro.

The inhibition of BTZ-resistant DprE1 followed the trend observed in the MIC measurements, with the C387 g mutant being more resistant to inhibition by PyrBTZ01, PyrBTZ02, and BTZ043 (7- to 9-fold increases in IC50) than the C387S mutant (2.5- to 4-fold increases in IC50).

BTZ-043 was administered at 100 mg/kg (b.i.d., p.o.), and sulfamethoxazole/trimethoprim (SXT), at 100 mg/kg sulfamethoxazole, was used as a positive control.

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C17H16F3N3O5S

431.39

DMSO:13.3 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years