Table 2.
The anti-AChE and anti-BChE activity of novel spiroindolin-1,2-diazepine derivitives, 5a-v[a].
 | ||||||
|---|---|---|---|---|---|---|
| BChE | AChE | |||||
| Compound | R1 | R2 | % inhibition at 50 µM | IC50 (µM) | % inhibition at 50 µM | IC50 (µM) |
| 5a | 5-Cl | 4- CH3 | 18.12 ± 2.88 | – | 5.37 ± 3.11 | – |
| 5b | 5-Cl | 4-OCH3 | 36.84 ± 2.10 | – | 42.84 ± 2.15 | – |
| 5c | 5-Cl | 3,4-diCH3 | 36.97 ± 3.78 | – | Not active | – |
| 5d | 5- Cl | 2,5-diOCH3 | 19.19 ± 4.07 | – | 27.82 ± 5.26 | – |
| 5e | 5- Cl | 4-Cl | Not active | – | 13.40 ± 3.34 | – |
| 5f | 5-NO2 | 2-CH3 | 23.30 ± 3.97 | – | 59.63 ± 6.75 | 22.38 ± 2.11 |
| 5g | 5-NO2 | 4-CH3 | 24.41 ± 2.96 | – | 66.26 ± 6.57 | 5.88 ± 0.84 |
| 5h | 5-NO2 | 3,4-diCH3 | Not active | – | 48.57 ± 2.70 | – |
| 5i | 5-NO2 | 4-OCH3 | 31.20 ± 3.65 | – | 46.09 ± 3.38 | – |
| 5j | 5-NO2 | 2,5-diOCH3 | 58.43 ± 3.55 | 17.37 ± 3.29 | 61.68 ± 3.77 | 20.89 ± 2.96 |
| 5k | 5-NO2 | 4-Cl | 17.89 ± 1.81 | – | 24.64 ± 1.70 | - |
| 5l | 5-NO2 | 4-OH | 5.71 ± 2.82 | – | 87.39 ± 5.93 | 3.98 ± 1.07 |
| 5m | 5,7-diCl | 2-CH3 | 41.94 ± 6.47 | – | 24.76 ± 5.48 | – |
| 5n | 5,7-diCl | 4-OCH3 | 46.50 ± 4.77 | – | 35.36 ± 7.54 | – |
| 5o | 5,7-diBr | 4-CH3 | 14.07 ± 3.70 | – | 37.57 ± 4.74 | – |
| 5p | 5,7-diBr | 2,5-diOCH3 | 59.26 ± 3.15 | 37.85 ± 4.85 | 73.36 ± 4.21 | 11.32 ± 1.65 |
| 5q | 5,7-diBr | 3-OH | 37.15 ± 0.84 | - | 63.13 ± 4.43 | 12.03 ± 2.33 |
| 5r | 5,7-diBr | 4-OH | 51.66 ± 1.29 | 45.70 ± 5.62 | 46.70 ± 1.92 | - |
| 5s | 7-CF3 | 4-OCH3 | 13.38 ± 3.46 | – | 56.05 ± 4.39 | 17.78 ± 2.79 |
| 5t | 7-CF3 | 2-CH3 | 7.31 ± 5.07 | – | 24.72 ± 1.94 | - |
| 5u | 7-CF3 | 3-OH | 10.45 ± 1.07 | – | 16.39 ± 0.53 | - |
| 5v | 7-CF3 | 4-OH | 13.03 ± 1.14 | – | 17.74 ± 1.82 | - |
| Donepezil[b] | 10.6 ± 2.1 | 0.079 ± 0.05 | ||||
[a]Data presented here are the mean ± S.E of three to five independent experiments.
[b]Positive control.