Table 7. Rat Liver-Isolated MAO (rMAO) Inhibitory Activity of Donepezil–Propargylamine–8-Hydroxyquinoline Derivatives.
compound | X | n | IC50 for MAO-A (μM) | IC50 for MAO-B (μM) | SI valuea |
---|---|---|---|---|---|
56 | H | 0 | ≥100 | ≥100 | 1 |
57 | CN | 1 | 22.1 ± 0.7 | 39.5 ± 1.4 | 0.559 |
58 | H | 1 | 85.4 ± 3.7 | 19.4 ± 3.2 | 4.402 |
59 | CN | 2 | 9.7 ± 1.5 | 12.4 ± 2.5 | 0.782 |
60 | H | 2 | ≥100 | 50.1 ± 5 | 1.996 |
61 | CN | 3 | 6.2 ± 0.7 | 10.2 ± 0.9 | 0.607 |
62 | H | 3 | ≥100 | 34.5 ± 3.5 | 2.898 |
Selectivity index for MAO-B (IC50 for MAO-A/IC50 for MAO-B).