Table 1.
Inhibitory activity of compounds 3a–3h towards AChE and BuChE and radical scavenging ability.
| Compound | AChE IC50 ± SD [nM] a |
BuChE IC50 ± SD [nM] b |
Selectivity for AChE c | Selectivity for BuChE d | ORAC (TE) e |
|---|---|---|---|---|---|
| 3a | 8619.37 ± 606.33 | 539.92 ± 66.90 | 0.063 | 15.96 | n.d. |
| 3b | 272.33 ± 35.11 | 103.73 ± 7.63 | 0.38 | 2.62 | 0.4614 ± 0.056 |
| 3c | 272.79 ± 22.11 | 200.20 ± 18.07 | 0.73 | 1.36 | n.d. |
| 3d | 4057.16 ± 535.79 | 173.41 ± 18.89 | 0.043 | 23.39 | n.d. |
| 3e | 394.69 ± 36.07 | 194.88 ± 11.02 | 0.49 | 2.02 | n.d. |
| 3f | 113.34 ± 7.14 | 203.52 ± 16.02 | 1.79 | 0.56 | 0.3254 ± 0.014 |
| 3g | 700.98 ± 67.08 | 177.63 ± 17.03 | 0.25 | 3.95 | n.d. |
| 3h | 669.42 ± 83.39 | 226.97 ± 27.05 | 0.34 | 2.95 | n.d. |
| Tacrine | 226.97 ± 27.05 | 7.2 ± 0.51 | 0.032 | 31.52 | 0.0132 ± 0.009 |
| Bistacrine | 405.10 ± 28.62 | 226 ± 30.40 | 0.56 | 1.79 | n.d. |
a IC50: 50% inhibitory concentration (means ± SD of three independent experiments) of AChE. b IC50: 50% inhibitory concentration (means ± SD of three independent experiments) of BuChE. c Selectivity for AChE: IC50(BuChE)/IC50(AChE). d Selectivity for BuChE: IC50(AChE)/IC50(BuChE). e Data are expressed as Trolox equivalents (TE) and are shown as mean ± SD. n.d.: not determined.