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. 2019 Dec 6;35(1):298–305. doi: 10.1080/14756366.2019.1697250

Table 1.

Inhibition data of human CA isoforms hCA I, II, IX and XII for the target sulphonamides (4a,b, 5a,b, 9a–c, and 10a–d), using (AAZ) as a standard drug.

Inline graphic
Compound R R1 KI (nM)*
hCA I hCA II hCA IX hCA XII
4a H 162.8 12.3 33.3 26.9
4b Br 92.7 73.5 48.4 38.8
5a H 37.4 33.6 60.4 10.1
5b Br 63.9 44.2 27.7 32.5
9a H CH3 1292 643.7 32.8 49.7
9b Br H 2159 888.2 44.6 33.4
9c Br CH3 2503 571.1 10.0 16.7
10a H H 4625 353.9 76.6 71.8
10b H CH3 3921 228.5 51.1 38.9
10c Br H 1822 438.8 85.4 66.8
10d Br CH3 827.6 727.1 97.5 27.5
AAZ 250.0 12.0 25.0 5.7
*

Mean from three different assays, by a stopped flow technique (errors were in the range of ±5–10% of the reported values).