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. 2017 Sep 11;32(1):1174–1182. doi: 10.1080/14756366.2017.1368019

Table 3.

AChE, human carbonic anhydrase I, and II isoforms (hCA I, and II) AChE and BChE enzymes inhibition effects of aminomethyl and alkoxymethyl derivatives (1–17) and proportion of AChE to BChE enzymes.

  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.

a

Acetazolamide (AZA) was used as a standard inhibitor for both carbonic anhydrase I, and II isoenzymes (hCA I and II).