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).