Table 9. Inhibitory Activity of hMAO Isoenzymes by Donepezil–Coumarin Hybrids.
compound | R1 | R2 | n | m | IC50 for MAO-B (μM) |
---|---|---|---|---|---|
73 | H | H | 2 | 0 | 8.39 ± 0.91 |
74 | H | H | 3 | 0 | 12.6 ± 1.2 |
75 | H | H | 2 | 2 | 30.4 ± 2.5 |
76 | H | Me | 2 | 0 | 2.75 ± 0.22 |
77 | H | Cl | 2 | 0 | 33.9 ± 2.1 |
78 | H | OMe | 2 | 0 | 33.6 ± 0.9 |
79 | H | OEt | 2 | 0 | 31.9 ± 1.9 |
80 | H | CF3 | 2 | 0 | 28.5 ± 1.7 |
81 | H | Ph | 2 | 0 | 45.6 ± 3.6 |
82 | Me | H | 2 | 0 | 2.38 ± 0.11 |
83 | Me | Me | 2 | 0 | 23.4 ± 1.1 |
84 | Cl | Me | 2 | 0 | 14.7 ± 1.5 |
85 | –(CH2)4– | 2 | 0 | 2.62 ± 0.81 | |
86 | H | Me | 0 | 1.93 ± 0.33 | |
87 | H | Me | 2 | 40.5 ± 4.1 |