TABLE 1.
Inhibitory activity of the target compounds 3a-t against AChE and BuChE.
| |||||
|---|---|---|---|---|---|
| Compound | nc | R | R′ | AChE IC50 (nM)a | BuChE IC50 (nM)b |
| 3a | 3 | H | H | 4.0 ± 0.0 | 84.0 ± 4.0 |
| 3b | 3 | 6-OMe | H | 4.0 ± 1.0 | 68.0 ± 6.0 |
| 3c | 3 | 7-OMe | H | 7.0 ± 1.0 | 57.0 ± 10.0 |
| 3d | 3 | 8-OMe | H | 81.0 ± 4.0 | 79.0 ± 9.0 |
| 3e | 3 | 6-Br | H | 15.0 ± 3.0 | 33.0 ± 5.0 |
| 3f | 3 | 6-NO2 | H | 2.0 ± 0.0 | 24.0 ± 5.0 |
| 3g | 4 | H | H | 7.0 ± 1.0 | 91.0 ± 18.0 |
| 3h | 4 | 6-OMe | H | 1003 ± 37.0 | 106.0 ± 8.0 |
| 3i | 4 | 7-OMe | H | 144.0 ± 9.0 | 46.0 ± 1.0 |
| 3j | 4 | 8-OMe | H | 31.0 ± 5.0 | 97.0 ± 19.0 |
| 3k | 4 | 6-Br | H | 40.0 ± 5.0 | 92.0 ± 9.0 |
| 3l | 4 | 6-NO2 | H | 3.0 ± 1.0 | 59.0 ± 11.0 |
| 3m | 5 | H | H | 72.0 ± 8.0 | 86.0 ± 10.0 |
| 3n | 5 | 8-OMe | H | 15.0 ± 2.0 | 123.0 ± 24.0 |
| 3o | 5 | 6-NO2 | H | 22.0 ± 4.0 | 27.0 ± 2.0 |
| 3p | 5 | 6-Br | H | 3.0 ± 0.0 | 49.0 ± 5.0 |
| 3q | 5 | 6-Br | 5-Ethyl-2-Methyl | 19.0 ± 1.6 | 22.0 ± 2.3 |
| 3r | 5 | 6-Br | 4-Dimethylamine | 26.0 ± 2.1 | 52.0 ± 3.6 |
| 3s | 3 | H | 4-Dimethylamine | 22.0 ± 1.9 | 34.0 ± 2.6 |
| 3t | 3 | 6-NO2 | 4-Dimethylamine | 14.0 ± 0.9 | 9.0 ± 0.4 |
| Donepezil | 14.0 ± 3.0 | 2,750 ± 205.0 | |||
a
Inhibitor concentration (mean ± SEM of three experiments) required for 50% inactivation of AChE (electric eel).
b
Inhibitor concentration (mean ± SEM of three experiments) required for 50% inactivation of BuChE (equine serum).
c
Length of linker (n = 3, 4, 5).