Table 1. Inhibitory Effects against VchCAα, VchCA-β, VchCA-γ, hCA I, and hCA II of Compounds 20a–i and Reference Compound Acetazolamide (AAZ).
|
Ki (nM) |
|||||
|---|---|---|---|---|---|
| VchCAα | VchCβ | VchCAγ | hCA I | hCA II | |
| 20a | 45.0 | 6442.0 | 56.1 | 60.7 | 3.3 |
| 20b | 9.1 | 626.7 | 250.8 | 65.9 | 5.1 |
| 20c | 8.8 | 3596.0 | 722.4 | 77.8 | 31.6 |
| 20d | 18.1 | 179.2 | 98.4 | 95.0 | 63.0 |
| 20e | 11.6 | 95.6 | 174.6 | 2113.0 | 919.7 |
| 20f | 12.1 | 586.1 | 657.4 | 98.3 | 54.4 |
| 20g | 6.2 | 553.9 | 593.0 | 269.3 | 26.3 |
| 20h | 10.0 | 200.4 | 775.0 | 44.2 | 83.8 |
| 20i | 7.7 | 538.5 | 79.6 | 571.5 | 69.5 |
| AAZ | 6.8 | 451.0 | 470.0 | 250.0 | 12.1 |
a
Errors in the range of ±10% of the reported value, from 3 different assays.