Table 2. Influence of the substitution in the benzylic position and modified analogues at the amide bond of the synthetic macamides on TNF-α.
| No. | Derivatives | Viability (CC50 μM) THP-1 cells | TNF-α inhibition (IC50 μM) THP-1 cells | clog P a |
| 2a |
|
98.1 ± 1.84 | 8.9 ± 0.98 | 7.40 |
| 2b |
|
95.8 ± 1.97 | 5.2 ± 0.81 | 8.20 |
| 2c |
|
96.5 ± 1.79 | 19.7 ± 1.94 | 8.29 |
| 2d |
|
98.0 ± 1.46 | 56.8 ± 1.75 | 7.29 |
| 2e |
|
97.3 ± 1.94 | 13.1 ± 1.74 | 8.33 |
| 2f |
|
89.1 ± 1.23 | 23.8 ± 1.44 | 8.11 |
| 2g |
|
95.4 ± 1.88 | 6.4 ± 0.91 | 8.10 |
| 2h |
|
84.3 ± 1.12 | 5.3 ± 0.75 | 8.17 |
| 2i |
|
98.7 ± 1.97 | 1.6 ± 0.07 | 8.30 |
| 2j |
|
95.0 ± 1.82 | 0.97 ± 0.02 | 8.31 |
aValues of clog P were calculated by DataWarrior.27