Table 1. hCA I, II, IX, and XII Inhibition Data of the Newly Synthesized Sulfonamides 4a–9b and Acetazolamide AAZ as Standard, by the Stopped Flow CO2 Hydrase Assay24.
|
Ki (nM)a |
||||
|---|---|---|---|---|
| compd | hCA I | hCA II | hCA IX | hCA XII |
| 4a | 5.3 | 5.0 | 8.3 | 7.2 |
| 4b | 6.6 | 5.1 | 5.8 | 6.5 |
| 4c | 41.2 | 5.7 | 7.7 | 6.6 |
| 4d | 7.9 | 5.5 | 7.1 | 5.7 |
| 4e | 6.1 | 5.2 | 6.9 | 6.4 |
| 5a | 649 | 66.5 | 8.7 | 88.5 |
| 5b | 452 | 36.6 | 17.9 | 9.6 |
| 5c | 286 | 8.9 | 32.6 | 7.5 |
| 5d | 52.5 | 8.8 | 6.6 | 7.3 |
| 5e | 63.0 | 3.9 | 6.5 | 6.5 |
| 7a | 18.0 | 5.0 | 8.5 | 8.6 |
| 7b | 17.1 | 4.6 | 7.2 | 5.7 |
| 7c | 90.9 | 3.9 | 8.8 | 7.1 |
| 9a | 826 | 215 | 9.6 | 609 |
| 9b | 151 | 43.3 | 7.9 | 36.7 |
| AAZ | 250 | 12.1 | 25.0 | 5.7 |
a
Mean from three different assays; errors are in the range of ±10% of the reported value.