Table 1.
eeAChEa |
eqBuChEb |
|||||
---|---|---|---|---|---|---|
Compd. | n | R | R1 | R2 | IC50 (μM)/Inhibition (%) | IC50 (μM)/Inhibition (%) |
4a | 2 | A | H | H | 45.3 ± 0.35% | 16.69 ± 2.36% |
4b | 3 | A | H | H | 3.96 ± 0.71 μM | 16.60 ± 4.01% |
4c | 4 | A | H | H | 0.22 ± 0.03 μM | 45.37 ± 8.34% |
4d | 5 | A | H | H | 0.24 ± 0.02 μM | 20.95 ± 2.61% |
4e | 6 | A | H | H | 0.35 ± 0.02 μM | 17.49 ± 2.17% |
4f | 4 | B | H | H | 0.69 ± 0.22 μM | 37.22 ± 1.22% |
4g | 4 | C | H | H | 9.61 ± 1.12 μM | 31.43 ± 3.15% |
4h | 4 | D | H | H | 3.80 ± 0.35 μM | 2.00 ± 0.23 μM |
4i | 4 | E | H | H | 20.17 ± 3.27% | 15.81 ± 2.45% |
4j | 4 | F | H | H | 14.52 ± 2.44% | 23.91 ± 2.03% |
4k | 4 | G | H | H | 23.14 ± 5.54% | 28.65 ± 3.44% |
4l | 4 | H | H | H | 12.31 ± 1.76% | 30.47 ± 4.11% |
4m | 4 | I | H | H | 31.43 ± 1.65% | 7.63 ± 0.92% |
9a | 4 | A | Me | H | 0.30 ± 0.12 μM | 18.31 ± 3.15% |
9b | 4 | A | Me | Me | 0.34 ± 0.01 μM | 21.20 ± 1.60% |
Donepezil | – | – | – | – | 0.041 ± 0.002 μM | 4.22 ± 0.20 μM |
Galanthamine | – | – | – | – | 1.65 ± 0.14 μM | 11.68 ± 3.49 μM |
Tacrine | – | – | – | – | 0.21 ± 0.02 μM | 0.057 ± 0.013 μM |
aThe 50% inhibitory concentration of eeAChE or percent inhibition with inhibitor at 10 μM (means ± SD of three experiments).
bThe 50% inhibitory concentration of eqBuChE or percent inhibition with inhibitor at 10 μM (means ± SD of three experiments).