Table 1.
Inhibitory activity (%) of compounds 4a–4u against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes at 10−4 M concentration and their half maximal inhibitory concentration (IC50; µM) values against these enzymes.
| AChE (Electrophorus electricus) (%) ± SD |
AChE (Human) (%) ± SD |
BChE (Equine) (%) ± SD |
BChE (Human) (%) ± SD |
|||||
|---|---|---|---|---|---|---|---|---|
| Compound | 10−4 M | IC50 (µM) | 10−4 M | IC50 (µM) | 10−4 M | IC50 (µM) | 10−4 M | IC50 (µM) |
| 4a | 17.03 ± 0.48 | - | 18.15 ± 0.51 | - | * 91.13 ± 2.94 | 0.226 ± 0.008 | * 93.25 ± 2.24 | 0.243 ± 0.009 |
| 4b | 32.41 ± 1.01 | - | 35.49 ± 1.00 | - | * 82.50 ± 2.07 | 0.264 ± 0.012 | * 84.18 ± 2.21 | 0.222 ± 0.010 |
| 4c | 5.11 ± 0.09 | - | 10.28 ± 0.22 | - | 22.70 ± 0.70 | - | 20.55 ± 0.61 | - |
| 4d | 31.64 ± 0.45 | - | 34.71 ± 0.77 | - | 40.19 ± 0.49 | - | 45.26 ± 0.60 | - |
| 4e | 7.09 ± 0.64 | - | 10.13 ± 0.51 | - | * 95.98 ± 2.88 | 1.420 ± 0.068 | * 96.57 ± 2.03 | 1.373 ± 0.057 |
| 4f | 4.70 ± 0.27 | - | 8.71 ± 0.62 | - | 12.80 ± 0.87 | - | 15.67 ± 0.79 | - |
| 4g | 10.44 ± 0.66 | - | 11.30 ± 0.58 | - | 33.65 ± 0.89 | - | 35.97 ± 0.80 | - |
| 4h | 15.23 ± 0.69 | - | 18.39 ± 0.57 | - | 12.64 ± 0.46 | - | 15.58 ± 0.67 | - |
| 4i | 35.91 ± 1.57 | - | 33.85 ± 1.15 | - | * 69.51 ± 1.16 | 2.038 ± 0.068 | * 72.90 ± 1.08 | 2.097 ± 0.085 |
| 4j | 2.88 ± 0.18 | - | 5.97 ± 0.22 | - | 27.86 ± 1.07 | - | 30.77 ± 1.20 | - |
| 4k | 8.62 ± 0.22 | - | 7.21 ± 0.18 | - | 25.14 ± 1.42 | - | 20.65 ± 1.20 | - |
| 4l | 3.90 ± 0.09 | - | 7.29 ± 0.18 | - | 45.88 ± 1.62 | - | 42.60 ± 1.53 | - |
| 4m | 25.43 ± 1.21 | - | 27.38 ± 1.10 | - | * 98.96 ± 3.47 | 0.092 ± 0.001 | * 97.50 ± 2.06 | 0.093 ± 0.002 |
| 4n | * 63.21 ± 1.76 | 45.945 ± 1.581 | * 68.39 ± 1.99 | 41.129 ± 1.694 | * 99.03 ± 3.26 | 0.015 ± 0.0006 | * 98.25 ± 2.63 | 0.014 ± 0.0005 |
| 4o | 25.30 ± 1.01 | - | 30.45 ± 1.15 | - | * 74.83 ± 2.17 | 1.071 ± 0.051 | * 75.25 ± 2.08 | 1.069 ± 0.039 |
| 4p | 48.40 ± 1.18 | - | 49.51 ± 1.50 | - | 48.65 ± 1.14 | - | 40.71 ± 1.08 | - |
| 4q | 16.35 ± 0.39 | - | 20.28 ± 0.51 | - | 39.90 ± 1.36 | - | 42.48 ± 1.22 | - |
| 4r | 37.33 ± 1.03 | - | 40.70 ± 1.00 | - | 45.30 ± 1.88 | - | 43.29 ± 1.17 | - |
| 4s | 32.17 ± 1.23 | - | 35.20 ± 1.12 | - | 38.40 ± 0.74 | - | 34.99 ± 0.63 | - |
| 4t | 15.94 ± 0.42 | - | 14.51 ± 0.44 | - | * 55.00 ± 1.74 | 1.515 ± 0.072 | * 54.26 ± 1.27 | 1.607 ± 0.062 |
| 4u | 25.88 ± 0.74 | - | 30.71 ± 0.52 | - | 29.50 ± 0.48 | - | 31.21 ± 0.50 | - |
| Aminoacridine | 75.18 ± 1.15 | 1.752 ± 0.072 | 78.22 ± 0.89 | 1.339 ± 0.047 | 87.29 ± 1.07 | 0.233 ± 0.009 | 86.12 ± 1.22 | 0.221 ± 0.007 |
| Donepezil | 98.56 ± 2.87 | 0.0077 ± 0.0003 | 96.95 ± 2.14 | 0.0072 ± 0.0002 | 71.65 ± 2.16 | 1.683 ± 0.064 | 76.50 ± 2.08 | 1.419 ± 0.047 |
| Tacrine | 97.29 ± 3.24 | 0.147 ± 0.004 | 98.79 ± 2.63 | 0.151 ± 0.002 | 98.61 ± 3.71 | 0.0068 ± 0.0002 | 99.15 ± 2.07 | 0.0070 ± 0.0002 |
* Represents the selected compounds for second step due to more than 50% inhibitory potency at 10−4 M concentration.