Table 8. hMAO Enzyme Inhibition Activity of Donepezil–Picolinamide Hybrids.
compound | R | n | IC50 FOR MAO-A (μM) | IC50 FOR MAO-B (μM) | SI valuea |
---|---|---|---|---|---|
63 | 2-Br-Ph-CH2 | 2 | NA | 46.8 ± 2.2 | |
64 | 3-NO2–Ph | 2 | 92.4 ± 7.1 | 26.2 ± 1.5 | 3.526 |
65 | 4-NO2–Ph | 2 | 22.6 ± 1.8 | 68.3 ± 4 | 0.330 |
66 | 4-CH3–Ph | 2 | NA | 94.1 ± 4.9 | |
67 | 4-Cl-Ph | 2 | 23.2 ± 1.8 | 9.27 ± 1.3 | 2.502 |
68 | 2-quinoline | 2 | 24.5 ± 2.3 | 48.6 ± 3.3 | 0.504 |
69 | 5-Cl-2-pyridine | 2 | 13.4 ± 0.9 | 3.14 ± 0.27 | 4.267 |
70 | 6-CH3-2-pyridine | 2 | NA | 2.53 ± 1.4 | |
71 | 5-Cl-2-thiophene | 2 | 76.4 ± 5.4 | 11.5 ± 0.9 | 6.643 |
72 | 5-Br-2-thiophene | 2 | 96.2 ± 4.8 | 9.47 ± 0.54 | 10.158 |
Selectivity index for MAO-B (IC50 for MAO-A/IC50 for MAO-B).