Table 1.
Cholinesterase inhibition IC50 average ±SD of BOPs and donepezil hydrochloride.
 | |||||
|---|---|---|---|---|---|
| Compound | R | R1 | X | AChE Inhibition [IC50 (μM)] | BuChE Inhibition [IC50 (μM)] |
| BOP-1 | H | 3-Br | Br | 5.90 ± 0.07 | 6.76 ± 0.04 |
| BOP-2 | H | 4-Cl | Cl | 47.14 ± 0.48 | 29.04 ± 0.43 |
| BOP-3 | H | 4-F | Cl | >100 | 70.43 ± 0.41 |
| BOP-4 | H | 4-CN | Br | >100 | >100 |
| BOP-5 | H | H | Br | 41.21 ± 0.62 | 12.63 ± 0.11 |
| BOP-6 | OMe | 3-Br | Br | 6.77 ± 0.24 | 8.77 ± 0.11 |
| BOP-7 | OMe | 4-F | Cl | 21.92 ± 0.2 | >100 |
| BOP-8 | OMe | 4-Cl | Cl | 1.11 ± 0.09 | >100 |
| BOP-9 | OMe | 4-CN | Br | >100 | >100 |
| BOP-10 | OMe | H | Br | 10.08 ± 0.28 | 18.84 ± 0.34 |
| BOP-11 | OMe | 4-CN | Br | >100 | >100 |
| BOP-12 | OMe | 4-Cl | Cl | >100 | >100 |
| Donepezil | - | - | - | 0.079 ± 0.002 | 5.19 ± 0.38 |
Bold value signifies the most active compounds related IC50 values.