Table 2.
Inhibitory activity of 3a–3p against Mtb H37Ra.
| Compound | R3 | MIC (µg/mL) | CLogP a |
|---|---|---|---|
| 3a |
|
50 | 4.67 |
| 3b |
|
100 | 5.52 |
| 3c |
|
100 | 5.68 |
| 3d |
|
10 | 3.63 |
| 3e |
|
25 | 3.01 |
| 3f |
|
5 | 3.54 |
| 3g |
|
5 | 4.24 |
| 3h |
|
2.5 | 4.48 |
| 3i |
|
1.25 | 5.04 |
| 3j |
|
1.25 | 5.60 |
| 3k b |
|
1.25 | 5.56 |
| 3l |
|
0.625 | 6.08 |
| 3m b |
|
25 | 6.88 |
| 3n b |
|
25 | 2.95 |
| 3o |
|
100 | 3.06 |
| 3p |
|
100 | 3.33 |
| INH | 0.1 |
a CLogP was calculated with ChemBioDraw Ultra 12.0. b The compound was obtained as a mixture of trans- and cis-isomers.