Table 1. Inhibition of hCA Isoforms I, II, IX and XII with Compounds 1a–d and 2a–d.
Ki (μM)a |
||||
---|---|---|---|---|
compd | hCA Ib | hCA IIb | hCA IXc | hCA XIIc |
1a | 0.042 ± 0.0001 | 1820 ± 9 | 7.79 ± 0.06 | 7.78 ± 0.04 |
1b | 5.33 ± 0.04 | 4.70 ± 0.01 | 4.51 ± 0.03 | 0.34 ± 0.006 |
1c | 4.83 ± 0.07 | 0.70 ± 0.008 | 18.9 ± 0.21 | 0.28 ± 0.01 |
1d | 6.61 ± 0.02 | 0.78 ± 0.009 | 2.91 ± 0.04 | 0.44 ± 0.005 |
2a | 4.31 ± 0.06 | 6.95 ± 0.08 | 0.47 ± 0.003 | 0.57 ± 0.008 |
2b | 5.93 ± 0.06 | 0.53 ± 0.003 | 7.90 ± 0.08 | 0.35 ± 0.002 |
2c | 6.45 ± 0.03 | 0.76 ± 0.05 | 7.36 ± 0.04 | 0.21 ± 0.01 |
2d | 0.62 ± 0.005 | 0.41 ± 0.007 | 3.02 ± 0.008 | 0.31 ± 0.01 |
AAZ | 0.25 ± 0.01 | 0.012 ± 0.001 | 0.025 ± 0.002 | 0.006 ± 0.0005 |
MZA | 0.78 ± 0.04 | 0.014 ± 0.001 | 0.027 ± 0.008 | 0.034 ± 0.002 |
DCP | 1.2 ± 0.1 | 0.038 ± 0.003 | 0.050 ± 0.005 | 0.050 ± 0.004 |
Errors in the range of ±5–10% of the reported value from three different determinations.
Full length.
Catalytic domain. AAZ, acetazolamide; MZA, methazolamide; DCP, dichlorophenamide.