Table 1.
Inhibitory effects of the prepared compounds against MAO-B enzyme.
| Comp. | C5 Linker | R (C5 Substitution) | N1 Indole Substitution | % Inhibition of MAO-B at 10 µM |
|---|---|---|---|---|
| 4a |
|
|
3-Fluorobenzoyl | 46.2 ± 1.1 |
| 4b |
|
9.9 ± 1.5 | ||
| 4c |
|
26.6 ± 0.6 | ||
| 4d |
|
44.0 ± 0.8 | ||
| 4e |
|
47.9 ± 1.6 | ||
| 4f |
|
32.5 ± 1.4 | ||
| 4g |
|
55.7 ± 0.2 | ||
| 4h |
|
38.6 ± 1.6 | ||
| 4i |
|
37.0 ± 0.9 | ||
| 4j |
|
53.5 ± 0.3 | ||
| 4k |
|
42.1 ± 1.7 | ||
| 4l |
|
42.0 ± 0.6 | ||
| 4m |
|
38.1 ± 0.5 | ||
| 4n |
|
32.9 ± 0.3 | ||
| 5a |
|
|
3-Fluorobenzoyl | 15.5 ± 1.1 |
| 5b |
|
45.6 ± 1.2 | ||
| 5c |
|
43.9 ± 1.1 | ||
| 5d |
|
46.8 ± 0.2 | ||
| 5e |
|
44.7 ± 0.5 | ||
| 5f |
|
34.1 ± 0.7 | ||
| 5g |
|
30.6 ± 0.9 | ||
| 5h |
|
32.5 ± 0.5 | ||
| 5i |
|
59.8 ± 0.4 | ||
| 5j |
|
51.1 ± 0.4 | ||
| 6a |
|
|
3-Fluorobenzoyl | 26.8 ± 1.3 |
| 6b |
|
33.8 ± 2.3 | ||
| 6c |
|
35.5 ± 1.5 | ||
| 6d |
|
53.0 ± 0.3 | ||
| 6e |
|
59.6 ± 0.3 | ||
| 7a |
|
|
3-Fluorobenzoyl | 49.8 ± 0.3 |
| 7b |
|
3,4-Dichlorobenzoyl | 84.1 ± 0.0 | |
| 8a |
|
|
Free NH | 99.3 ± 0.0 |
| 8b |
|
99.4 ± 0.0 | ||
| 8c |
|
34.2 ± 0.2 | ||
| 8d |
|
15.3 ± 0.8 | ||
| 8e |
|
89.6 ± 0.4 |