Table 1.
Dual agents endowed with NO donating properties and selective hCA isoform inhibitory activity for the treatment of open-angle glaucoma.
Compound | Structure | Ki (nM) | ||
---|---|---|---|---|
hCA I | hCA II | hCA IV | ||
Dorzolamide | ![]() |
50,000 | 3.2 | 43 |
Isosorbide mononitrate | ![]() |
>100,000 | >100,000 | >100,000 |
1 | ![]() |
2950 | 14 | 4360 |
2 | ![]() |
470 | 71 | 46 |
3 | ![]() |
410 | 13 | 181 |
4 | ![]() |
705 | 76 | 339 |
5 | ![]() |
1520 | 63 | 3905 |
6 | ![]() |
189 | 18 | 44 |
7 | ![]() |
242 | 198 | 345 |
8 | ![]() |
15 | 10 | 47 |
9 | ![]() |
40 | 28 | 154 |
10 | ![]() |
137 | 33 | 225 |
11 | ![]() |
32 | 10 | 46 |
12 | ![]() |
43 | 14 | 38 |
13 | ![]() |
395 | 101 | 139 |
14 | ![]() |
587 | 88 | 148 |
15 | ![]() |
41 | 12 | 76 |
16 | ![]() |
950 | 71 | 89 |
17 | ![]() |
>100,000 | >100,000 | nd |
18 | ![]() |
>100,000 | >100,000 | nd |
19 | ![]() |
>100,000 | >100,000 | nd |
20 | ![]() |
>100,000 | >100,000 | nd |
21 | ![]() |
>100,000 | >100,000 | nd |
22 | ![]() |
>100,000 | >100,000 | nd |
23 | ![]() |
>100,000 | >100,000 | nd |
24 | ![]() |
>100,000 | >100,000 | nd |
25 | ![]() |
>100,000 | >100,000 | nd |
26 | ![]() |
>100,000 | >100,000 | nd |
27 | ![]() |
>100,000 | >100,000 | nd |
28 | ![]() |
>100,000 | >100,000 | nd |
Dichlorophenamide | ![]() |
1200 | 38 | 15,000 |
Acetazolamide | ![]() |
250 | 12 | 74 |
nd: not determined.