Table 1.

Profiling of diazaborine and oxaborole inhibitors of M. tuberculosis InhA.

Cpd IDStructureMWInhA inhibition (μM) (IC50)H37Rv (μM) IC90THP-1 intracellular IC50 (μM)THP-1 intracellular IC90 (μM)THP-1 cytotoxicity IC50 (μM)HepG2 cytotoxicity IC50 (μM)
AN2918Embedded Image294.044>200 (n = 2)
AN3438Embedded Image294.11216 ± 1.2 (n = 3)
AN6534Embedded Image341.27936 ± 1.7 (n = 3)
AN12541Embedded Image427.20.400.11 ± 0.21 (n = 5)0.046 ± 0.013 (n = 2)0.11 ± 0.01 (n = 2)>50 (n = 1)>100 (n = 3)
AN12855Embedded Image441.20.0300.090 ± 0.050 (n = 10)0.021 ± 0.003 (n = 3)0.04 ± 0.01 (n = 3)>50 (n = 2)>100 (n = 3)
AN12908Embedded Image441.22.37.0 ± 2.6 (n = 3)
  • MW, molecular weight.