Table 1 Inhibitory activity (IC50, μM) of conjugates of aminoadamantanes with carbazole derivatives C-1 and C-2 (Fig. 1) towards AChE, BChE and CaE.
Compounds | IC50 (μM) ± SEM or (inhibition % at 20 μM) | |||||
|---|---|---|---|---|---|---|
No | R | R1 | R2 | AChE | BChE | CaE |
C-1a | H | H | H | >20 (2.8%) | 15.9 ± 1.0 | >20 (9.3%) |
C-1b | H | H | CH3 | n.a. | 7.6 ± 0.3 | >20 (10.5%) |
C-1c | Br | Br | H | >20 (5.5%) | 20.7 ± 0.2 | >20 (25.3%) |
C-1d | Br | Br | CH3 | >20 (6.1%) | 55.4 ± 4.9 | n.a. |
C-1e | CI | CI | H | >20 (13.1%) | 23.7 ± 0.4 | 50.1 ± 4.8 |
C-1f | CI | CI | CH3 | >20 (4.0%) | 40.7 ± 3.2 | n.a. |
C-2a | H | H | H | >20 (4.6%) | 7.29 ± 0.50 | >20 (17.9%) |
C-2b | H | H | CH3 | >20 (5.1%) | 6.13 ± 0.40 | >20 (10.1%) |
C-2c | CH3 | H | H | >20 (3.9%) | 20.02 ± 1.18 | >20 (15.1%) |
C-2d | CH3 | H | CH3 | >20 (2.2%) | 33.0 ± 0.2 | >20 (12.3%) |
C-2e | CH3 | CH3 | H | >20 (7.1%) | 9.17 ± 0.74 | >20 (20.0%) |
C-2f | CH3 | CH3 | CH3 | >20 (7.3%) | 8.24 ± 0.36 | >20 (10.3%) |
C-2g | F | H | H | >20 (4.9%) | 8.66 ± 0.32 | >20 (15.4%) |
C-2h | F | H | CH3 | >20 (8.8%) | 5.43 ± 0.39 | >20 (16.5%) |
Memantine | >20 (1.3%) | >20 (13.7%) | >20 (3.0%) | |||
Amantadine | >20 (3.4%) | >20 (6.9%) | >20 (3.2%) | |||
Carbazole | >20 (1.8%) | >20 (16.1%) | >20 (9.4%) | |||
Tacrine | 0.60 ± 0.05 | 0.0290 ± 0.0002 | n.a. | |||
BNPP | n.a. | n.a. | 1.80 ± 0.11 | |||
