Table 5.
IC50 and SI for selected salicylanilide 4-(trifluoromethyl)benzoates 1.
| R1 | R2 | IC50 [µmol/L] HepG2 | SI for Mtb. H37Rv 331/88 | SI for MDR-TB strains | SI for XDR-TB strain | SI for Staphylococcus sp. | |||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 24 h | 14 d | 21 d | 14 d | 21 d | 14 d | 14 d | 24 h | 48 h | |||
| 1e | 4-Cl | 3,4-diCl | 3.13 | 3.13 | 3.13 | 1.57–3.13 | 0.78–1.57 | 1.57 | 1.57 | 6.39 | 3.19 |
| 1f | 5-Cl | 3,4-diCl | 4.46 | 4.46 | 2.23 | 2.23–4.46 | 2.23 | 4.46 | 2.23 | - | - |
| 1g | 4-Cl | 3-Br | 2.63 | 2.63 | 1.32 | 1.32–2.63 | 1.32 | 2.63 | 1.32 | - | - |
| 1j | 5-Cl | 4-Br | 4.82 | 2.41 | 1.21 | 2.24 | 2.24 | 4.82 | 2.41 | 9.84 | 4.92 |
| 1o | 4-Cl | 4-CF3 | 1.33 | 1.33 | 1.33 | 1.33–2.66 | 1.33–2.66 | 2.66 | 1.33 | 0.34 | 0.17 |
| 1p | 5-Cl | 4-CF3 | 1.77 | 0.89 | 0.89 | - | - | - | - | 3.61 | 1.81 |
| 1r | 4-Br | 4-CF3 | 2.03 | 2.03 | 2.03 | 2.03–4.06 | 1.02–2.03 | 4.06 | 2.03 | - | - |
| SAL-1 | 5-Cl | 3,4-diCl | 0.84 | 0.21 | 0.10 | - | - | - | - | - | - |
| SAL-2 | 4-Cl | 3,4-diCl | 1.80 | 0.45 | 0.45 | - | - | - | - | - | - |
| SAL-3 | 5-Cl | 3-Br | 1.54 | NT | NT | - | - | - | - | - | - |
| SAL-4 | 4-Cl | 4-Br | 1.98 | 0.5 | 0.5 | - | - | - | - | - | - |
| SAL-5 | 5-Cl | 4-CF3 | 0.36 | 0.18 | 0.18 | - | - | - | - | - | - |
| SAL-6 | 4-Cl | 4-CF3 | 0.69 | 0.17 | 0.17 | - | - | - | - | - | - |
| SAL-7 | 5-Br | 4-CF3 | 1.67 | 1.67 | 1.67 | - | - | - | - | - | - |
| CF3-BA | 563.70 | - | - | - | - | - | - | - | - | ||
CF3-BA = 4-(trifluoromethyl)benzoic acid. SI = IC50/MIC100; MIC values of salicylanilides against M. tuberculosis were taken from reference [23].