Table 1.
Inhibition of CA isozymes I–XV (of human = h, and murine = m origin) with compounds 1–10.
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KI (μM)a,b |
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| No. | X | hCA I | hCA II | hCA III | hCA IV | hCA VA | hCA VB | hCA VI | hCA VII | hCA IXc | hCA XIIc | mCA XIII | hCA XIV | mCA XV |
| 1 | OH | 8.65 | 9.30 | 6.63 | 9.10 | 80.9 | 79.8 | 8.80 | 7.93 | 9.55 | 6.45 | 8.72 | 8.79 | 8.03 |
| 2 | NH2 | 0.086 | 0.101 | 2.26 | 7.96 | 1.68 | 8.82 | 0.097 | 0.095 | 0.097 | 0.090 | 0.100 | 0.092 | 0.100 |
| 3 | NHNH2 | 9.8 | 5.31 | 6.28 | 78.4 | 7.75 | 95.2 | 74.4 | 8.56 | 51.7 | 2.42 | 5.96 | 3.81 | 5.16 |
| 4 | NHOH | 2.73 | 5.47 | 4.42 | 24.6 | 5.28 | 67.9 | 86.2 | 8.73 | 60.3 | 1.53 | 4.97 | 1.66 | 7.17 |
| 5 | NHOMe | >1000 | 8.96 | 5.72 | 39.5 | 6.70 | 10.7 | 27.0 | 9.56 | 64.3 | 8.32 | 6.21 | 1.57 | 7.84 |
| 6 | OH | 730 | 30.1 | 35.7 | 434 | 7.12 | 9.60 | 91.6 | 92.2 | 66.5 | 20.4 | 44.8 | 0.98 | 72.8 |
| 7 | NH2 | 324 | 93.2 | 35.7 | 381 | 46.8 | 83.1 | 82.6 | 76.8 | 3.67 | 11.2 | 45.1 | 27.0 | 85.5 |
| 8 | NHNH2 | 91.2 | 231 | 40.2 | 335 | 59.3 | 75.9 | 63.5 | 76.7 | 48.4 | 45.0 | 44.4 | 0.99 | 94.2 |
| 9 | NHOH | 83.1 | 179 | 44.8 | 84.7 | 67.4 | 53.6 | 78.1 | 70.7 | 45.9 | 9.51 | 23.0 | 0.94 | 79.9 |
| 10 | NHOMe | 72.5 | 341 | 37.3 | 111 | 89.1 | 57.3 | 89.9 | 72.2 | 57.5 | 28.5 | 63.3 | 10.0 | 106 |
aErrors in the range of ±5% of the reported data from three different assays.
bh = human; m = murine isozyme.
cCatalytic domain.
