TBA-7371

TBA-7371 is an orally active and non-covalent inhibitor of Decaprenylphosphoryl-β-D-ribose oxidase (DprE1) of Mycobacterium tuberculosis (MIC=0.64 μg/mL). TBA-7371 can block the synthesis of arabinose in the bacterial cell wall, resulting in cell wall structural defects, thereby exerting an anti-tuberculosis effect. TBA-7371 can be used in the research of anti-tuberculosis drugs and has a synergistic bactericidal effect with Bedaquiline (HY-14881) and other drugs^[1][2][3]. IC50 & Target:DprE1^[1] In Vitro:The MIC of TBA-7371 against Erdman and H37Rv strains of Mycobacterium tuberculosis is 1 μg/mL. In the presence of 4% human serum albumin, the MIC increases only 2-fold, indicating that binding to human serum albumin had little effect^[2].
TBA-7371 (1, 10, 100 μg/mL; 14 days) shows dose-dependent bactericidal activity against Erdman strain of Mycobacterium tuberculosis, with the 100 μg/mL group showing the most significant bactericidal effect^[2]. In Vivo:TBA-7371 (100, 200 mg/kg; oral gavage; twice daily; 4-8 weeks) synergistically exerts bactericidal and fungicidal activity with Bedaquiline (HY-14881) and GSK2556286 (HY-147017) in the BALB/c mouse tuberculosis model^[3].
TBA-7371 (50, 100, 200 mg/kg; oral gavage; twice daily; 8 weeks) significantly reduces bacterial burden in lung tissue after 8 weeks of treatment in the C3HeB/Fe J mouse tuberculosis model^[3].