Table 4.
The enzyme inhibition data of human carbonic anhydrase isoenzymes (hCA-I and -II) with the most active pyrazole, pyrazolo[1,5-a]pyrimidine derivatives, and Acetazolamide.
Compound No. | hCA-I | hCA-II | ||
---|---|---|---|---|
IC50 (nM) | Ki (nM) | IC50 (nM) | Ki (nM) | |
3a | 92.34 | 88.78 | 73.2 | 91.85 |
5a | 137.99 | 176.21 | 161.22 | 144.27 |
6 | 168.84 | 153.46 | 130.29 | 145.58 |
9a | 123.41 | 101.55 | 142.28 | 135.78 |
10a | 153.45 | 143.59 | 121.98 | 139.37 |
ACZ a | 994.78 | 1052.22 | 900.33 | 981.64 |
a: Acetazolamide was used as a standard inhibitor for both CA-I and CA-II isoenzymes (hCA-I and -II).