Table 3.
IC50 (nM) |
Ki (nM) |
||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Compounds | hCA I | r2 | hCA II | r2 | AChE | r2 | BChE | r2 | hCA I | hCA II | AChE | BChE | AChE/BChE |
1 | 79 | 0.9639 | 104 | 0.9527 | 51 | 0.9762 | 88 | 0.9964 | 108 ± 35 | 81 ± 19 | 26 ± 5 | 32 ± 7 | 0.812 |
2 | 79 | 0.9852 | 114 | 0.9839 | 39 | 0.9885 | 89 | 0.9773 | 77 ± 15 | 107 ± 11 | 33 ± 5 | 51 ± 4 | 0.647 |
3 | 83 | 0.9597 | 89 | 0.9555 | 54 | 0.9670 | 75 | 0.9619 | 106 ± 39 | 96 ± 22 | 37 ± 11 | 45 ± 9 | 0.822 |
4 | 86 | 0.9588 | 99 | 0.9774 | 36 | 0.9855 | 82 | 0.9630 | 86 ± 40 | 105 ± 25 | 18 ± 2 | 41 ± 13 | 0.439 |
5 | 82 | 0.9755 | 98 | 0.9670 | 52 | 0.9699 | 83 | 0.9359 | 70 ± 15 | 100 ± 24 | 34 ± 9 | 51 ± 9 | 0.666 |
6 | 102 | 0.9359 | 118 | 0.9649 | 44 | 0.9857 | 80 | 0.9750 | 123 ± 48 | 115 ± 28 | 45 ± 11 | 30 ± 3 | 1.500 |
7 | 79 | 0.9597 | 116 | 0.9457 | 65 | 0.9874 | 79 | 0.9520 | 82 ± 17 | 132 ± 27 | 40 ± 8 | 57 ± 17 | 0.701 |
8 | 94 | 0.9533 | 119 | 0.9619 | 38 | 0.9848 | 48 | 0.9911 | 58 ± 15 | 121 ± 40 | 32 ± 6 | 23 ± 3 | 1.391 |
9 | 103 | 0.9652 | 121 | 0.9440 | 62 | 0.9769 | 84 | 0.9904 | 76 ± 20 | 135 ± 33 | 78 ± 36 | 80 ± 9 | 0.975 |
10 | 98 | 0.9550 | 137 | 0.9452 | 50 | 0.9819 | 94 | 0.9710 | 99 ± 22 | 135 ± 42 | 61 ± 9 | 50 ± 10 | 1.220 |
11 | 112 | 0.9607 | 172 | 0.9711 | 89 | 0.9865 | 133 | 0.9621 | 118 ± 40 | 137 ± 35 | 45 ± 5 | 77 ± 17 | 0.584 |
12 | 119 | 0.9752 | 141 | 0.9695 | 63 | 0.9908 | 93 | 0.9947 | 95 ± 25 | 146 ± 46 | 75 ± 8 | 88 ± 11 | 0.852 |
13 | 105 | 0.9664 | 122 | 0.9483 | 63 | 0.9859 | 83 | 0.9807 | 90 ± 23 | 94 ± 37 | 34 ± 5 | 35 ± 4 | 0.971 |
14 | 112 | 0.9426 | 128 | 0.9556 | 38 | 0.9860 | 68 | 0.9704 | 119 ± 53 | 142 ± 56 | 23 ± 4 | 60 ± 13 | 0.383 |
15 | 128 | 0.9783 | 158 | 0.9644 | 43 | 0.9888 | 109 | 0.9752 | 118 ± 27 | 193 ± 79 | 25 ± 3 | 45 ± 14 | 0.555 |
16 | 156 | 0.9757 | 167 | 0.9659 | 76 | 0.9949 | 127 | 0.9590 | 132 ± 30 | 162 ± 29 | 42 ± 4 | 55 ± 12 | 0.763 |
17 | 142 | 0.9774 | 187 | 0.9562 | 80 | 0.9912 | 144 | 0.9749 | 157 ± 38 | 215 ± 40 | 54 ± 10 | 42 ± 20 | 1.285 |
AZA a | 373 | 0.9774 | 520 | 0.9816 | — | — | — | — | 333 ± 28 | 353 ± 60 | — | — | — |
TACb | — | — | — | — | 174 | 0.9513 | 280 | 0.9879 | — | — | 109 ± 5 | 128 ± 16 | 0.851 |
Tacrine (TAC) was used as a standard inhibitor for BChE and AChE enzymes.
Acetazolamide (AZA) was used as a standard inhibitor for both carbonic anhydrase I, and II isoenzymes (hCA I and II).