Table 1.
Results of the evaluation of the inhibitory activities of the compounds on cholinesterases.
| AChE | BChE | |||
|---|---|---|---|---|
| Compound | % Inhibition a |
Ki (µM) [Ki′ (µM)] (type of inhibition) |
% Inhibition a |
Ki (µM) [Ki′ (µM)] (type of inhibition) |
| Galantamine hydrobromide | 96.7 | 0.2 ± 0.1 (competitive) | 86.3 | 2.4 ± 0.0 (competitive) |
| Xylofuranos-5′-yl isonucleosides | ||||
| Purine derivatives | ||||
| 4 | 16.3 | n.d. | 11.9 | n.d. |
| 5 | 25.3 | n.d. | 32.5 | n.d. |
| Uracil derivatives | ||||
| 6 | 22.5 | n.d. | 28.5 | n.d. |
| 7 | 17.8 | n.d. | 7.5 | n.d. |
| 8 | 26.1 | n.d. | 32.8 | n.d. |
| 9 | 40.3 | 17.5 ± 0.7 [103.0 ± 4.3] (mixed-type) |
29.8 | n.d. |
| Theobromine derivatives | ||||
| 3 | 13.8 | n.d. | 11.7 | n.d. |
| 10 | 2.6 | n.d. | 22.9 | n.d. |
| 13-α | 18.9 | n.d. | 35.0 | n.d. |
| 18 | 14.5 | n.d. | 19.6 | n.d. |
| Glucopyranos-6′-yl theobromine isonucleoside | ||||
| 21 | 66.5 | 3.1 ± 0.2 [>100] (mixed-type) |
75.1 | 5.4 ± 0.3 [>60] (mixed-type) |
| Theobromine-containing isonucleotide analogs | ||||
| 12 | 1.0 | n.d. | 4.6 | n.d. |
| 15 | 12.4 | n.d. | 35.9 | n.d. |
| 22 | 28.3 | n.d. | 52.6 | n.d. |
a % Inhibition at 50 µM. AChE, acetylcholinesterase; BChE, butyrylcholinesterase.