Table 1.
Human CA isoenzymes (hCA I and II) inhibition value of the compounds (9–16) by the esterase method with 4-nitrophenyl acetate as substrate.
IC50 (nM) |
Ki (nM) |
|||||
---|---|---|---|---|---|---|
Compounds | hCA I | r2 | hCA II | r2 | hCA I | hCA II |
9 | 554.8 | 0.9759 | 586.3 | 0.9723 | 506.3 ± 133.5 | 624.6 ± 168.2 |
10 | 491.8 | 0.9816 | 620.4 | 0.9565 | 476.5 ± 81.1 | 561.5 ± 133.9 |
11 | 483.9 | 0.9743 | 486.3 | 0.9688 | 533.1 ± 187.8 | 469.0 ± 63.0 |
12 | 402.9 | 0.9646 | 559.3 | 0.9814 | 377.6 ± 113.8 | 520.6 ± 131.8 |
13 | 493.2 | 0.9709 | 536.0 | 0.9737 | 462.2 ± 133.5 | 587.3 ± 188.5 |
14 | 404.8 | 0.9817 | 470.5 | 0.9602 | 316.7 ± 9.6 | 412.5 ± 115.4 |
15 | 416.5 | 0.9815 | 534.3 | 0.9631 | 325.8 ± 29.4 | 430.3 ± 87.3 |
16 | 528.2 | 0.9710 | 458.6 | 0.9772 | 472.0 ± 57.5 | 591.9 ± 134.5 |
AZA | 985.8 | 0.9811 | 489.4 | 0.9972 | 278.8 ± 44.3 | 293.4 ± 46.4 |
Acetazolamide (AZA) was used as a standard inhibitor for all hCA isoenzymes. The results were expressed as nanomolar (nM).