Table 4.
In vitro antitubercular activity of series 4 compounds.[a]
|
||||||||
|---|---|---|---|---|---|---|---|---|
| Compd | R1 | R2 | R3 | MIC | CC50 [b] | |||
| μg mL−1 | μm | μg mL−1 | μm | |||||
| 30 a |
|
|
Br | 1.0 | 2.0 | 10 | 20.1 | |
| 30 b |
|
|
Br | 2.0 | 3.9 | 3.8 | 7.4 | |
| 30 c |
|
|
Br | 1.8 | 3.5 | 12 | 23.4 | |
| 30 d |
|
|
Br | 1.6 | 3.3 | 25 | 51.9 | |
| 30 e |
|
|
OMe | 1.8 | 4.0 | 12 | 26.7 | |
| 30 f |
|
|
H | 2.0 | 4.9 | 15 | 37.1 | |
| 30 g |
|
|
H | >32 | 76.5 | >64 | >153.1 | |
| 30 h |
|
|
Br | >32 | >75.1 | >64 | >150.2 | |
| 30 i |
|
|
Br | >32 | >73.7 | >64 | >147.5 | |
| 30 j |
|
|
Br | 1.6 | 3.3 | 4.4 | 9.2 | |
| 30 k |
|
|
Br | 1.9 | 4.0 | 11 | 23.6 | |
| 30 l |
|
|
Br | 1.0 | 2.2 | 11 | 23.6 | |
| 30 m |
|
|
Br | >32 | >63.8 | >64 | >127.8 | |
| 30 n |
|
|
Br | >32 | >67.5 | 3.9 | 8.2 | |
[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 %.