Table 5.
In vitro antitubercular activity of compounds from the second round of optimization.[a]
|
||||||
|---|---|---|---|---|---|---|
| Compd | R | MIC | CC50 [b] | |||
| μg mL−1 | μm | μg mL−1 | μm | |||
| 32 a |
|
0.43 | 0.87 | 13 | 26.1 | |
| 32 b |
|
1.9 | 3.7 | 6.3 | 12.3 | |
| 32 c |
|
1.7 | 3.2 | 4.1 | 7.6 | |
| 32 d |
|
0.47 | 0.87 | 12 | 22.3 | |
| 32 e |
|
0.44 | 0.73 | 3.9 | 6.6 | |
| 32 f |
|
2.2 | 3.9 | 4.8 | 8.6 | |
| 32 g |
|
1.5 | 2.3 | >64 | >101.9 | |
| 32 h |
|
0.61 | 1.0 | 4.6 | 7.5 | |
| 32 i |
|
3.4 | 6.3 | 3.8 | 7.0 | |
| 32 j |
|
10 | 15.6 | 36 | 56.3 | |
| 32 k |
|
0.73 | 1.2 | 53 | 87.9 | |
| 32 l |
|
0.84 | 1.6 | 40 | 77.7 | |
| 32 m |
|
1.4 | 2.7 | 14 | 27.1 | |
| 32 n |
|
0.79 | 1.5 | 3.7 | 7.0 | |
| 32 o |
|
0.67 | 1.3 | 12 | 22.7 | |
| 32 p |
|
0.51 | 0.94 | 13 | 24.1 | |
| 32 q |
|
1.1 | 2.1 | 17 | 32.7 | |
| 32 r |
|
3.1 | 5.7 | >64 | >118.7 | |
| 32 s |
|
>32 | >62.3 | >64 | >124.5 | |
| 32 t |
|
>32 | >60.9 | >64 | >121.9 | |
| 32 u |
|
>32 | >62.9 | >64 | >125.7 | |
| 32 v |
|
>32 | >59.8 | 44 | 82.2 | |
[a] Reference compound: bedaquiline MIC=0.060 μg mL−1 (0.1 μm). [b] Concentration at which the growth of Vero cells is inhibited by 50 %.