Table 6.
The in vitro activity (MIC values in μM units) of investigated compounds 1a–p and reference drugs isoniazid (INH), ethambutol (EMB), ofloxacin (OFLX) and ciprofloxacin (CPX) against M. tuberculosis CNCTC My 331/88 (M. tuberculosis H37Rv; MTv H37Rv), M. tuberculosis H37Ra ATCC 25177 (MTa H37Ra), M. kansasii CNCTC My 235/80 (MK 235/80), M. kansasii 6509/96 (MK 6509/96) and M. kansasii DSM 44162 (MK DSM), respectively.
| Comp. | MIC [μM] | |||||||||
|---|---|---|---|---|---|---|---|---|---|---|
|
MTv H37Rv |
MTa H37Ra |
MK 235/80 | MK 6509/96 |
MK DSM |
||||||
| 1 14-d | 2 21-d | 3 7-d | 7-d | 14-d | 21-d | 7-d | 14-d | 21-d | 7-d | |
| 1a | 32 | 32 | 213 | 62.5 | 62.5 | 62.5 | 32 | 62.5 | 62.5 | 53 |
| 1b | 16 | 32 | 52 | 32 | 32 | 62.5 | 32 | 32 | 62.5 | 26.1 |
| 1c | 16 | 16 | 25 | 32 | 32 | 32 | 16 | 16 | 16 | 12.7 |
| 1d | 8 | 8 | 12.5 | 16 | 16 | 32 | 8 | 16 | 16 | 6.2 |
| 1e | 16 | 32 | 8.1 | 32 | 32 | 32 | 16 | 16 | 32 | 16.2 |
| 1f | 16 | 16 | <3.9 | 16 | 16 | 32 | 8 | 16 | 16 | 7.9 |
| 1g | 8 | 16 | <3.8 | 16 | 16 | 16 | 8 | 8 | 16 | 3.8 |
| 1h | 4 | 8 | <3.7 | 8 | 8 | 8 | 4 | 4 | 8 | 1.9 |
| 1i | 16 | 32 | 203 | 32 | 62.5 | 62.5 | 16 | 32 | 32 | 51 |
| 1j | 16 | 32 | 199 | 16 | 32 | 62.5 | 16 | 32 | 32 | 50 |
| 1k | 8 | 16 | 195 | 16 | 32 | 62.5 | 16 | 32 | 32 | 98 |
| 1l | 4 | 8 | 96 | 16 | 32 | 32 | 16 | 16 | 32 | 382 |
| 1m | 8 | 16 | 15.4 | 16 | 16 | 32 | 8 | 16 | 16 | 7.7 |
| 1n | 4 | 8 | 7.5 | 8 | 8 | 8 | 4 | 8 | 8 | 7.5 |
| 1o | 8 | 16 | 7.3 | 8 | 16 | 16 | 4 | 8 | 8 | 3.6 |
| 1p | 4 | 8 | 7.1 | 8 | 8 | 8 | 4 | 8 | 8 | 3.6 |
| INH | 0.5 | 1 | 36.5 | >250 | >250 | >250 | 2 | 4 | 8 | 29.2 |
| EMB | 1 | 2 | – | – | – | – | 1 | 2 | 2 | – |
| OFLX | 1 | 2 | – | 0.5 | 1 | 1 | 0.5 | 0.5 | 1 | – |
| CPX | – | – | 48.3 | – | – | – | – | – | – | 3.0 |
1 14-d, 14-Day cultivation; 2 21-d, 21-day cultivation; 3 7-d, 7-day cultivation. The most promising values of compounds in vitro antimycobacterial activity (MIC ≤ 8 μM) were indicated in gray cells of Table 6.