Table 1.
Compound | IC50 (nM) AChE a | IC50 (nM) BuChE b | Selectivity Index c | Aβ (1–42) Aggregation Inhibition (%) d | |
---|---|---|---|---|---|
8a | 306.5 ± 12.4 | 202.9 ± 35.7 | 0.660 | 26.1 ± 4.5 | |
8b | 90.3 ± 7.3 | 119.7 ± 12.5 | 1.326 | 19.5 ± 2.7 | |
8c | 52.7 ± 8.2 | 215.4 ± 33.7 | 4.087 | 18.5 ± 4.0 | |
8d | 61.7 ± 5.2 | 106.9 ± 13.1 | 1.733 | 37.2 ± 0.9 | |
8e | 184.1 ± 15.2 | 195.7 ± 3.5 | 1.059 | 35.1 ± 3.2 | |
tacrine | 151.1 ± 10.3 | 27.6 ± 7.3 | 0.182 | n.t. e | |
curcumin | n.t. | n.t. | n.t. | 37.3 ± 1.2 | |
ferulic acid | n.t. | n.t. | n.t. | 36.5 ± 3.6 |
a Inhibitor concentration (mean ± SD of three independent experiments) required for 50% inactivation of AChE. b Inhibitor concentration (mean ± SD of three independent experiments) required for 50% inactivation of BuChE. c Selectivity index = IC50 (BuChE)/IC50 (AChE). d Inhibition of self-induced Aβ (1–42) aggregation, the thioflavin-T fluorescence method was used, the mean ± SD of at least three independent experiments and the measurements were carried out in the presence of 20 μM compounds. e n.t. = not tested.