Table 1. . Inhibition of recombinant human MAO-A and -B by harmine-conjugated 1,2,3-triazoles.
| Compounds | MAO-A IC50(μM) | MAO-B IC50(μM) | Selectivity index MAO-A/MAO-B |
|---|---|---|---|
| 2a | >100 | 30.76 ± 3.27 | – |
| 2b | 69.45 ± 2.53 | 8.21 ± 2.31 | 8.46 |
| 2c | 3.83 ± 0.04 | 43.65 ± 2.36 | 0.09 |
| 2d | >100 | >100 | – |
| 2e | 60.91 ± 0.62 | 38.29 ± 3.19 | 1.59 |
| 2f | 60.50 ± 3.09 | 39.65 ± 9.59 | 1.53 |
| 2g | 39.50 ± 1.50 | 21.32 ± 2.76 | 1.85 |
| 2h | 4.19 ± 0.16 | 58.08 ± 1.55 | 0.07 |
| 2i | >100 | 58.11 ± 11.45 | – |
| 3a | 3.61 ± 0.03 | 9.55 ± 1.19 | 0.38 |
| 3b | 1.53 ± 0.17 | 1.21 ± 0.14 | 1.26 |
| 3c | 7.78 ± 0.25 | 11.87 ± 3.50 | 0.66 |
| 3d | >100 | >100 | – |
| 3e | 0.83 ± 0.03 | 0.26 ± 0.04 | 3.20 |
| 3f | 3.94 ± 0.32 | 9.17 ± 0.04 | 0.43 |
| 3g | 1.69 ± 0.02 | 7.93 ± 0.38 | 0.21 |
| 4a | 1.30 ± 0.05 | 1.89 ± 0.02 | 0.69 |
| 4b | 1.40 ± .012 | 28.33 ± 0.58 | 0.05 |
| 4c | 0.43 ± 0.002 | 0.36 ± 0.001 | 1.20 |
| 4d | 1.32 ± 0.20 | 9.38 ± 0.48 | 0.14 |
| 5a | 1.46 ± 0.01 | 1.77 ± 0.26 | 0.82 |
| 5b | 2.68 ± 0.22 | 6.03 ± 0.89 | 0.44 |
| 5c | 9.26 ± 0.06 | 4.04 ± 0.52 | 2.29 |
| 5d | 0.51 ± 0.05 | 2.96 ± 0.23 | 0.17 |
| 5e | 0.86 ± 0.03 | 2.26 ± 0.72 | 0.38 |
| 5f | 0.56 ± 0.02 | 1.08 ± 0.02 | 0.52 |
| Harmine | 0.0043 ± 0.0003 | 22.33 ± 3.21 | 0.00019 |
| Clorgyline | 0.0048 ± 0.0006 | – | – |
| Deprenyl | – | 0.0530 ± 0.008 | – |
IC50 values are expressed as mean with mean ± SD of triplicate observations. Compounds with significant biological activity are highlighted as bold font.