Table 1. Inhibitory Profile of Compounds 2a–i against hCA I, II, IV, and VIIa.
Ki (nM) |
|||||
---|---|---|---|---|---|
compd | (Het)Ar | hCA I | hCA II | hCA IV | hCA VII |
2a | Ph | 466.1 | 376.5 | 3912.1 | 6.8 |
2b | 4-ClC6H4 | 453.0 | 182.1 | 608.2 | 0.96 |
2c | 4-FC6H4 | 428.7 | 742.2 | 1036.5 | 9.4 |
2d | 4-MeOC6H4 | 317.9 | 53.3 | 3643.4 | 0.97 |
2e | 2-MeC6H4 | 70.7 | 61.7 | 961.2 | 0.93 |
2f | 2-EtOC6H4 | 216.3 | 866.5 | 2299.7 | 0.84 |
2g | 3,4-(MeO)2C6H4 | 847.6 | 723.6 | 8302.6 | 0.87 |
2h | 3-pyridyl | 316.0 | 848.3 | 1826.6 | 0.84 |
2i | 5-pyrimidinyl | 274.5 | 703.2 | 2296.0 | 0.83 |
1a | 4-FC6H4 | 2343.0 | 76.1 | 9726.0 | 303.5 |
1b | 4-ClC6H4 | 960.5 | 46.7 | 8142.0 | 269.0 |
AAZ | 250.0 | 12.1 | 74.0 | 6.0 |
Mean Ki values from three different stopped-flow assays (errors were in the range of ±5–10% of the reported values). Inhibitory profile of compounds 1a–b23 is provided for comparison.