Table 1.
Cholinesterase inhibition (eeAChE, eqBChE) and antioxidative potential (DPPH, CUPRAC) of derivatives 1–14.
| Compound | eeAChE | eqBChE | DPPH | CUPRAC | |||
|---|---|---|---|---|---|---|---|
| IC50
(μM) |
Inhibition ** (%) |
IC50 (μM) | Inhibition ** (%) |
IC50 (μM) | Inhibition ** (%) |
mol TE/mol of Compound | |
|
177.7 | 80.9 ± 1.9 (500) | 66.0 | 83.5 ± 0.8 (400) | 159.2 | 77.2 ± 0.5 (500) | 0.925 |
|
82.3 | 83.0 ± 2.5 (250) | 53.0 | 80.4 ± 6.4 (200) | 265.1 | 65.0 ± 2.4 (500) | 0.713 |
|
404.6 | 77.8 ± 5.2 (500) | 206.4 | 68.5 ± 6.2 (500) | 36.2 | 87.7 ± 0.8 (500) | 1.111 |
|
225.0 | 82.1 ± 1.1 (250) | 36.5 | 81.1 ± 2.2 (250) | 51.4 | 90.3 ± 0.6 (400) | 0.852 |
|
154.9 | 84.6 ± 2.7 (250) | 22.9 | 75.3 ± 2.3 (100) | 130.3 | 83.0 ± 1.9 (400) | 0.204 |
|
27.1 | 82.4 ± 0.8 (80) | 39.7 | 84.0 ± 1.8 (100) | - * | 42.9 ± 2.7 (400) | 1.407 |
|
62.9 | 81.1 ± 1.1 (200) | 42.5 | 83.1 ± 0.8 (200) | 23.8 | 86.2 ± 2.3 (50) | 2.350 |
|
92.4 | 78.2 ± 7.7 (150) | 24.8 | 88.5 ± 5.0 (250) | 26.3 | 89.3 ± 1.2 (250) | 1.148 |
|
- * | 17.6 ± 3.1 (100) | - * | 10.5 ± 4.1 (250) | 428.4 | 55.4 ± 0.7 (500) | 1.000 |
|
- * | 34.2 ± 2.1 (500) | - * | 22.4 ± 9.0 (500) | - * | 24.0 ± 0.7 (500) | 0.630 |
|
- * | 29.3 ± 1.8 (500) | - * | 9.8 ± 2.7 (500) | 30.1 | 89.8 ± 0.0 (524) | n.d. *** |
|
- * | 9.1 ± 1.4 (500) | 189.5 | 68.4 ± 1.3 (500) | 139.8 | 74.1 ± 0.4 (524) | n.d. *** |
|
- * | 17.1 ± 3.9 (500) | 30.7 | 78.2 ± 3.8 (500) | 699.2 | 59.8 ± 2.3 (1047) | n.d. *** |
|
- * | 10.7 ± 2.4 (250) | - * | 15.6 ± 3.6 (250) | - * | 11.2 ± 2.7 (250) | n.d. *** |
| Resveratrol | n.d. *** | n.d. *** | 74.0 [48] | n.d. *** | |||
| Galantamine | 0.15 [48] | 7.9 [46] | n.d. *** | n.d. *** | |||
* Not achieved an IC50 value. ** The numbers shown in parentheses represent maximal concentrations tested in μM. *** Not determined.