Table 3. Inhibition Parameters of Synthesized Compounds on the Activity of hAChE and BuChE.
human erythrocytes
AChE |
horse serum BuChE |
selectivity |
||||
---|---|---|---|---|---|---|
inhibitor | Ki (μM) | IC50 (μM) | Ki (μM) | IC50 (μM) | from Ki | from IC50 |
donepezil | 0.010 ± 0.006 | 0.011 ± 0.008 | 2.140 ± 1.380 | 1.270 ± 0.410 | 214 | 120 |
13a,b | 2.822 ± 0.022 | 1.540 ± 0.090 | 10.611 ± 4.205 | 7.350 ± 0.130 | 4 | 5 |
14 | 4.224 ± 1.920 | 1.500 ± 0.23 | 5.613 ± 1.294 | 5.800 ± 0.050 | 1 | 4 |
15 | 0.355 ± 0.035 | 0.636 ± 0.209 | 6.480 ± 2.420 | 4.760 ± 0.041 | 18 | 7 |
16 | 1.980 ± 0.180 | 2.160 ± 0.760 | 8.460 ± 3.930 | 7.590 ± 0.03 | 4 | 4 |
17 | 0.035 ± 0.008 | 0.058 ± 0.033 | 2.440 ± 1.290 | 4.740 ± 0.750 | 71 | 81 |
18 | 0.260 ± 0.036 | 0.342 ± 0.029 | 1.140 ± 0.052 | 2.650 ± 0.617 | 4 | 8 |
19 | 1.835 ± 0.597 | 1.509 ± 0.510 | 3.099 ± 2.610 | 1.140 ± 0.090 | 2 | 1 |
20 | 0.029 ± 0.007 | 0.043 ± 0.007 | 3.140 ± 1.800 | 5.734 ± 0.130 | 110 | 132 |
21 | 0.980 ± 0.220 | 0.755 ± 0.025 | 7.254 ± 4.572 | 15.130 ± 0.025 | 7 | 20 |
22 | 0.554 ± 0.052 | 0.853 ± 0.052 | 3.490 ± 2.240 | 2.170 ± 1.330 | 6 | 3 |
23 | 119.490 ± 61.030 | 34.500 ± 18.470 | 3.888 ± 3.110 | 1.620 ± 0.004 | <1 | <1 |
24 | 17.230 ± 6.420 | 12.155 ± 0.225 | 2.378 ± 1.730 | 5.410 ± 0.120 | <1 | <1 |
25 | 39.670 ± 12.040 | 25.195 ± 21.720 | 4.328 ± 2.969 | 9.820 ± 0.200 | <1 | <1 |
26 | 18.200 ± 7.640 | 11.135 ± 0.054 | 6.437 ± 2.633 | 4.820 ± 0.002 | <1 | <1 |