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. 2019 Jun 20;34(1):1164–1171. doi: 10.1080/14756366.2019.1626375

Table 1.

Inhibition data of TcCA, LdCA and human CA I and II with sulfonamides reported here and the standard inhibitor acetazolamide (AAZ) by a stopped flow CO2 hydrase assay.

Compound R KI (μM)a
TcCA LdCA hCA I hCA II
4   0.08 0.21 0.91 0.24
6 0.16 0.34 4.35 0.18
7 2.52 4.68 4.79 0.84
8 0.24 0.46 6.18 0.61
9 C6H5 3.54 3.87 1.38 0.39
10 4-F-C6H4 4.79 8.49 2.92 0.46
11   10.7 6.57 >50 1.81
12 0.11 0.39 6.21 0.64
13 C6H5 0.32 1.06 >50 2.78
14 4-F-C6H4 0.46 0.98 5.39 0.53
15 4-CF3-C6H4 0.51 2.34 5.20 0.24
16 4-F-3-CH3-C6H3 0.38 2.96 7.58 0.21
17 C6F5 0.28 1.36 0.69 0.27
18 3-CH3O-C6H4 0.91 0.95 8.21 5.15
19 3,4-(OCH2O)-C6H3 1.02 2.03 >50 4.33
20 3,5-CH3-C6H3 0.69 1.86 8.33 0.45
21 3,5-CF3-C6H3 1.35 3.65 5.99 1.72
22 CH2CH2C6H5 0.74 0.86 9.29 3.08
23 CH2-(2-furyl) 0.41 1.02 >50 2.53
24 2,4,5-triacetoxy-6-acetoxymethyl-tetrahydro-pyran-3-yl 2.47 3.64 5.67 1.89
25 2,4,5-trihydroxy-6-hydroxymethyl-tetrahydro-pyran-3-yl 2.14 2.97 4.92 0.86
AAZ 0.06 0.09 0.25 0.012
a

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