Table 1. Inhibition Data toward hCA I, II, IX, XII, and hCOX 1 and 2 Isozymes of Compounds EMAC10111a–g.
|
Ki(μM) |
IC50 (μM) |
||||||
|---|---|---|---|---|---|---|---|
| Compound EMAC | R | hCA I | hCA II | hCA IX | hCA XII | hCOX-1 | hCOX-2 |
| 10111a | 4-Cl | 0.49 | 0.28 | 1.25 | 0.65 | * | 16.21 |
| 10111b | 2,4-Cl | 0.75 | 0.053 | 2.78 | 0.34 | * | 18.32 |
| 10111c | 4-Br | 3.46 | 0.32 | 2.44 | 0.80 | * | 19.73 |
| 10111d | 4-CH3 | 0.96 | 0.26 | 2.26 | 0.78 | * | * |
| 10111le | 4-OCH3 | 3.37 | 0.28 | 2.25 | 0.84 | * | 21.78 |
| 10111f | H | 8.02 | 3.10 | 3.54 | 0.30 | * | * |
| 10111g | // | 9.07 | 0.86 | 3.43 | 0.06 | * | 12.61 |
| Reference compounds | |||||||
| AAZ | / | 0.25 | 0.01 | 0.02 | 0.006 | / | / |
| Indomethacin | / | / | / | / | / | 12.16 | 35.20 |
| Diclofenac | / | / | / | / | / | 18.23 | 23.62 |
| FR122047 | / | / | / | / | / | 0.09 | ** |
| Nimesulide | / | / | / | / | / | *** | 23.14 |
| DuP 697 | / | / | / | / | / | 22.61 | 0.12 |
*
Inactive at 25 μM (highest concentration tested). At higher concentrations, the compounds precipitate.
**
Inactive at 100 μM (highest concentration tested). At higher concentrations, the compound precipitates.
***
Inactive at 500 μM (highest concentration tested). At higher concentrations, the compound precipitates.