Table 2. Inhibition Data of hCA I, hCA II, hCA VA, hCA VB, hCA VII, hCA IX, and hCA XII with Compounds 1b–3b, 5b–12b, 14b–20b, 4d, and 13e and the Standard Sulfonamide Inhibitor AAZ by a Stopped-Flow CO2 Hydrase Assay53.
| KI (nM)a | |||||||
|---|---|---|---|---|---|---|---|
| hCA I | hCA II | hCA VA | hCA VB | hCA VII | hCA IX | hCA XII | |
| 1b | 4666.7 | 9.3 | 59.1 | 141.3 | 51.6 | 6.2 | 78.9 |
| 2b | 4037.5 | 7.7 | 57.3 | 52.6 | 31.0 | 653.3 | 61.6 |
| 3b | >10,000 | 32.9 | 64.6 | 52.6 | 329.8 | 488.6 | 74.4 |
| 4d | >10,000 | 8.5 | 57.3 | 45.9 | 383.5 | 6557.1 | 74.0 |
| 5b | >10,000 | 70.7 | 59.4 | 42.9 | 281.1 | 8047.1 | 74.0 |
| 6b | 85.5 | 7.7 | 3217.2 | 22.6 | 688.5 | 240.1 | 40.4 |
| 7b | 28.0 | 1.3 | 4795.3 | 54.2 | 48.5 | 3.7 | 7.0 |
| 8b | 483.0 | 13.4 | 1469.3 | 29.0 | 9.5 | 85.5 | 7.8 |
| 9b | 289.7 | 6.3 | 3243.0 | 47.8 | 9.4 | >10,000 | 8.4 |
| 10b | 93.1 | 8.2 | 437.8 | 37.9 | 9.4 | 267.6 | 38.9 |
| 11b | 92.8 | 73.2 | 3972.2 | 45.0 | 66.0 | 373.2 | 9.0 |
| 12b | 62.3 | 5.6 | 6258.9 | 46.7 | 21.8 | >10,000 | 7.1 |
| 13e | 8771.0 | 21.3 | 3651.5 | 28.0 | 38.0 | >10,000 | 8.1 |
| 14b | >10,000 | >10,000 | 1725.8 | 44.0 | 0.7 | >10,000 | 8.7 |
| 15b | >10,000 | >10,000 | 57.8 | 161.0 | 9.3 | 6557.1 | 3.6 |
| 16b | >10,000 | >10,000 | 666.8 | 40.1 | 0.7 | 21.2 | 9.4 |
| 17b | >10,000 | >10,000 | 179.4 | 151.5 | 9.4 | 4885.7 | 3.5 |
| 18b | >10,000 | >10,000 | 301.8 | 42.7 | 0.6 | 2948.3 | 40.4 |
| 19b | >10,000 | >10,000 | 531.2 | 43.9 | 0.6 | >10,000 | 8.9 |
| 20b | >10,000 | >10,000 | 172.4 | 54.6 | 10.5 | 5852.3 | 2.8 |
| AAZ | 250.0 | 12.1 | 63.0 | 54.0 | 2.5 | 25.8 | 5.7 |
a
Mean from three different assays by a stopped-flow technique (errors were in the range of ±5–10% of the reported values).