Table 1.
Inhibition data of VChβ, FtuβCA, BpsCAβ, Can2, CgNce, MgCA and LdcCA with phenylphosphonic diamide 2 and alkyl phosphonamidates 3–10 and the standard sulphonamide inhibitor acetazolamide (AAZ) by a stopped flow CO2 hydrase assay29.
| |
KI (µM)a |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Compound | R | VChβ | FtuβCA | BpsCAβ | Can2 | CgNce | MgCA | LdcCA | CA I | CA II |
| 2 | – | 0.9 | 10.3 | 2.5 | 0.03 | 0.05 | 28.4 | 2.1 | 77.8 | 32.8 |
| 3 | –CH3 | 0.5 | 8.5 | 2.1 | 0.02 | 0.2 | 26.1 | 0.8 | 145.6 | 39.8 |
| 4 | –CH2CH3 | 9.5 | 16.4 | 4.6 | 0.05 | 0.8 | 68.1 | 3.5 | 338.6 | 160.6 |
| 5 | –(CH2)2CH3 | 15.4 | 35.6 | 12.6 | 0.9 | 1.3 | 79.0 | 6.8 | 589.9 | 459.4 |
| 6 | –CH(CH3)2 | 7.3 | 18.4 | 5.8 | 0.1 | 0.7 | 52.4 | 5.1 | 730 | 348.8 |
| 7 | –(CH2)3CH3 | 26.8 | 42.0 | 22.5 | 2.2 | 5.3 | 102.4 | 16.4 | 876.3 | 750 |
| 8 | –(CH2)2OCH3 | 64.9 | 55.3 | 29.4 | 10.4 | 8.7 | 265.7 | 36.5 | 961.2 | 520.1 |
| 9 | –(CH2)2Cl | 34.7 | 15.1 | 32.7 | 0.6 | 1.8 | 117.3 | 26.4 | 322.2 | 95.4 |
| 10 | –CH2CCH | 20.9 | 6.9 | 18.9 | 5.3 | 20.2 | 97.4 | 19.3 | 575.8 | 465.3 |
| AAZ | – | 0.45 | 0.77 | 0.74 | 0.01 | 0.01 | 40 | 0.09 | 0.25 | 0.01 |
a
Mean from three different assays, by a stopped flow technique (errors were in the range of ±5–10% of the reported values).