Table 2. Monoamine oxidase inhibition of pyrazolobenzothiazine-based carbothioamides 3a–o and 4a–o.
| Compound | MAO-A | MAO-B |
| IC50 ± SEM (μM) |
||
| 3a | 0.01 ± 0.0005 | 3.13 ± 0.14 |
| 3b | 0.003 ± 0.0007 | 29.5 ± 4.68 |
| 3c | 3.69 ± 0.04 | 4.15 ± 0.57 |
| 3d | 1.77 ± 0.03 | 2.91 ± 0.04 |
| 3e | 1.13 ± 0.001 | 0.11 ± 0.005 |
| 3f | 0.01 ± 0.0005 | 6.11 ± 0.07 |
| 3g | 4.06 ± 0.07 | 6.21 ± 0.09 |
| 3h | 1.11 ± 0.003 | 2.89 ± 0.07 |
| 3i | 3.49 ± 0.05 | 0.43 ± 0.006 |
| 3j | 1.42 ± 0.004 | 3.83 ± 0.03 |
| 3k | 0.47 ± 0.007 | 1.68 ± 0.005 |
| 3l | 30.2 ± 5.02 | 41% a |
| 3m | 76.2 ± 7.31 | 4.72 ± 0.38 |
| 3n | 64.8 ± 5.28 | 4.34 ± 0.06 |
| 3o | 31.2 ± 4.07 | 36% a |
| 4a | ND b | ND b |
| 4b | ND b | ND b |
| 4c | 27.2 ± 3.62 | 2.49 ± 0.03 |
| 4d | 8.18 ± 1.94 | 0.02 ± 0.001 |
| 4e | 9.15 ± 2.04 | 0.75 ± 0.004 |
| 4f | 65.7 ± 7.91 | 0.77 ± 0.005 |
| 4g | 33.8 ± 4.62 | 0.68 ± 0.003 |
| 4h | 7.73 ± 0.16 | 20.9 ± 2.74 |
| 4i | 2.06 ± 0.01 | 3.27 ± 0.04 |
| 4j | 0.54 ± 0.006 | 19% a |
| 4k | 9.02 ± 0.08 | 1.76 ± 0.008 |
| 4l | 2.33 ± 0.03 | 6.99 ± 0.05 |
| 4m | 10.6 ± 1.01 | 0.64 ± 0.007 |
| 4n | 3.07 ± 0.19 | 2.99 ± 0.06 |
| 4o | 0.97 ± 0.07 | 2.39 ± 0.05 |
| Clorgyline | 0.0045 ± 0.0003 | 61.35 ± 1.13 |
| Deprenyl | 67.25 ± 1.02 | 0.0196 ± 0.001 |
a% inhibition at 100 μM end concentration.
bND: not determined.