Table 1 Inhibitory activity (IC50) of conjugates of γ-carbolines and phenothiazine (Fig. 1) towards AChE, BChE and CaE.
Compounds | IC50 (μM) ± SEM | ||||
|---|---|---|---|---|---|
No | R1 | R2 | AChE | BChE | CaE |
C-1a | CH3 | CH3 | >200 | 62.6 ± 4.3 | >200 |
C-1b | CH3 | С2H5 | >200 | 2.04 ± 0.55 | >200 |
C-1c | F | CH3 | >200 | 1.79 ± 0.28 | >200 |
C-1d | H | CH3 | >200 | 1.07 ± 0.12 | >200 |
C-1e | H | С2H5 | >200 | 0.52 ± 0.01 | >200 |
C-1f | F | С2H5 | >200 | 0.58 ± 0.06 | >200 |
C-1g | С2H5 | CH3 | >100 | 1.36 ± 0.06 | >200 |
C-1h | i-С3H7 | CH3 | >100 | 2.79 ± 0.09 | 120 ± 13 |
C-2a | CH3 | CH3 | n.a. | 11.7 ± 0.4 | >200 |
C-2b | F | С2H5 | n.a. | 2.01 ± 0.04 | >200 |
C-2c | CH3O | CH3 | n.a. | 0.39 ± 0.02 | >200 |
dimebon | 36.3 ± 5.8 | 5.76 ± 0.51 | n.a. | ||
phenothiazine | n.a. | 137 ± 31 | n.a. | ||
МB | 1.21 ± 0.09 | 11.1 ± 0.1 | >200 | ||
BNPP | n.a. | n.a. | 1.80 ± 0.11 | ||
