Table 3. Influence of the aromatic ring and the position of methyl on the aromatic ring 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 |
| 3a |
|
93.2 ± 1.76 | 0.71 ± 0.03 | 8.64 |
| 3b |
|
94.7 ± 1.25 | 1.00 ± 0.03 | 8.07 |
| 3c |
|
90.9 ± 1.22 | 0.78 ± 0.02 | 8.45 |
| 3d |
|
93.5 ± 1.58 | 1.84 ± 0.03 | 8.00 |
| 3e |
|
93.6 ± 1.53 | 1.71 ± 0.03 | 8.14 |
| 3f |
|
95.0 ± 1.98 | 0.62 ± 0.03 | 8.31 |
| 3g |
|
82.3 ± 1.73 | 1.52 ± 0.04 | 7.99 |
| 3h |
|
82.5 ± 1.86 | 0.78 ± 0.03 | 8.04 |
| 3i |
|
81.4 ± 1.80 | 0.74 ± 0.03 | 8.37 |
| 3j |
|
89.8 ± 1.30 | 1.21 ± 0.04 | 8.52 |
| 3k |
|
92.5 ± 1.64 | 0.54 ± 0.03 | 8.20 |
| 3l |
|
91.7 ± 1.19 | 0.33 ± 0.02 | 8.31 |
| 3m |
|
93.2 ± 1.53 | 0.08 ± 0.001 | 8.50 |
aValues of clog P were calculated by DataWarrior.27