Table 6. hMAO Enzyme Inhibitory Activity of Donepezil–ASS234 Hybrids.
| compound | n | R1 | R2 | IC50 for MAO-A (μM) | IC50 for MAO-B (μM) | SI valuea |
|---|---|---|---|---|---|---|
| 40 | 0 | –Ph | –Me | >100 | >100 | 1 |
| 41 | 1 | –Ph | –Me | >100 | >100 | 1 |
| 42 | 2 | –Ph | –Me | >100 | >100 | 1 |
| 43 | 3 | –Ph | –Me | >100 | >100 | 1 |
| 44 | 0 | –Ph | –H | 14.1 ± 3.8 | >100 | 0.141 |
| 45 | 2 | –H | –Me | >100 | >100 | 1 |
| 46 | 0 | –H | –H | >100 | >100 | 1 |
| 47 | 2 | –H | –H | >100 | >100 | 1 |
| 48 | 4 | –Ph | –Me | 5.7 ± 2.1 | >100 | 0.057 |
| 49 | 2 | –Ph | –H | >100 | >100 | 1 |
| 50 | 3 | –Ph | –H | >100 | >100 | 1 |
| 51 | 4 | –Ph | –H | >100 | >100 | 1 |
| 52 | 3 | –H | –Me | >100 | 6.11 ± 1.4 | 16.366 |
| 53 | 4 | –H | –Me | >100 | 3.95 ± 0.94 | 25.316 |
| 54 | 3 | –H | –H | >100 | >100 | 1 |
| 55 | 4 | –H | –H | >50 | >50 | 1 |
Selectivity index for MAO-B (IC50 for MAO-A/IC50 for MAO-B).
