Table 2. In vitro inhibitory activity and selectivity index (SI) of clorsulon and acetazolamide (AAZ) as a reference sulfonamide-based drug against human CAs (hCA I, hCA II, hCA IX and hCA XII), schistosomal CA (SmCA) and other CAs belonging to different families, as assessed by a stopped-flow CO2-hydration assay (Khalifah, 1971 ▸).
| K i † (nM) | |||
|---|---|---|---|
| Clorsulon | AAZ | ||
| α-CAs | hCA I | 4516 | 250.0 |
| hCA II | 59.1 | 12.1 | |
| hCA IX | 137.5 | 25.7 | |
| hCA XII | 78.0 | 5.7 | |
| SmCA | 224.7 | 42.5 | |
| VhCAα | 291.7 | 6.8 | |
| SazCA | 7.7 | 0.9 | |
| β-CAs | VhCAβ | 906.1 | 6.8 |
| BpsCAβ | 223.3 | 745.0 | |
| mtCA 02 | 2.9 | 9.8 | |
| mtCA 03 | 827.5 | 104.0 | |
| γ-CA | BpsCAγ | 2500 | 149.0 |
| δ-CA | TweCA | 95.8 | 83.0 |
| SI (hCA I/SmCA) | 20.09 | 5.88 | |
Mean from three different assays using a stopped-flow technique (errors were in the range ±5–10% of the reported values).