Table 1.
Anti-TB activity of compounds 3a–w, 4–6 against M. tuberculosis strain H37Rv.
| Compd | MICMABA[a] [µg mL−1] |
MICBD[b] [µg mL−1] |
IC50 Vero cells[c] [µg mL−1] |
Compd | MICMABA [µg mL−1] |
MICBD [µg mL−1] |
IC50 Vero cells [µg mL−1] |
|---|---|---|---|---|---|---|---|
| 3a | 0.5 | 1.0 | 8.0 | 3n | >128 | nt | nt |
| 3b | >128 | >128 | nt[d] | 3o | 4.0 | nt | nt |
| 3c | >128 | >128 | nt | 3p | 4.0 | nt | nt |
| 3d | >128 | nt | nt | 3q | 0.5 | nt | nt |
| 3e | >128 | nt | nt | 3r | 0.5 | 1.0 | >64 |
| 3 f | 64 | nt | nt | 3s | 8.0 | nt | nt |
| 3g | 8.0 | nt | nt | 3t | >128 | nt | nt |
| 3h | 0.25 | 0.25 | >64 | 3u | 4.0 | nt | nt |
| 3i | 2.0 | 2.0 | 16 | 3v | 8.0 | nt | nt |
| 3j | 0.5 | nt | nt | 3w | >128 | nt | nt |
| 3k | 0.5 | nt | nt | 4 | 2.0 | nt | nt |
| 3l | 0.25 | 1.0 | 8.0 | 5 | 1.0 | nt | nt |
| 3m | 0.25 | 0.5 | 4.0 | 6 | >128 | nt | nt |
| INH[e] | 0.04 | nt | nt |
[a]
The lowest concentration of drug leading to at least a 90% reduction of bacterial growth signal by microplate Alamar Blue assay (MABA); values reported are the average of three individual measurements;
[b]
The lowest concentration of drug preventing visible bacterial growth in a 5 mL Tween-free Middlebrook broth dilution (BD) culture; values reported are the average of three individual measurements;
[c]
Cytotoxicity against Vero cells;
[d]
Not tested;
[e]
Isoniazid.