Table 2. In Vitro AChE Inhibitory Potency of Compounds 8, 10, 12–21, 23, and 28–33 and Donepezil.
compound no. | R | R′/Ar | IC50 (nM)a | relative potency (%) |
---|---|---|---|---|
8 | CH3 | 4-CH3C6H4 | 500.56 ± 14 | 10.99 |
10 | CH3 | 3,4-(CH3O)2C6H3 | 103.24 ± 2.8 | 53.27 |
12 | CH3 | 2,4-Cl2C6H3 | 335.79 ± 9.1 | 16.38 |
13 | CH3 | thiophen-2-yl | 173.75 ± 4.7 | 31.66 |
14 | CH3 | 5-bromothiophen-2-yl | 379.81 ± 10 | 14.48 |
15 | OCH3 | 4-CH3C6H4 | 374.70 ± 10 | 14.68 |
16 | OCH3 | 4-CH3OC6H4 | 108.94 ± 3 | 50.49 |
17 | OCH3 | 3,4-(CH3O)2C6H3 | 175.93 ± 4.8 | 31.26 |
18 | OCH3 | 4-ClC6H4 | 193.48 ± 5.3 | 28.43 |
19 | OCH3 | 2,4-Cl2C6H3 | 731.33 ± 20 | 7.52 |
20 | OCH3 | thiophen-2-yl | 259.64 ± 7.1 | 21.18 |
21 | OCH3 | 5-bromothiophen-2-yl | 187.83 ± 5.1 | 29.28 |
23 | 151.0 ± 4.1 | 36.42 | ||
28 | CH3 | CH3 | 478.20 ± 13 | 11.50 |
29 | CH3 | C6H5 | 187.86 ± 5.1 | 29.28 |
30 | OCH3 | CH3 | 346.40 ± 9.4 | 15.88 |
31 | OCH3 | C6H5 | 152.45 ± 4.1 | 36.08 |
32 | 3,4-(CH3O)2C6H3 | 450.4 ± 12 | 12.21 | |
33 | 2,4-Cl2C6H3 | 187.9 ± 5.1 | 29.27 | |
donepezil | 55.0 ± 0.004 | 100 |
Values are expressed as the mean ± standard error of the mean of three experiments.