Results of human MAO-A/MAO-B, and eeAChE/eqBChE and Aβ1–42 peptide aggregation inhibition.
| Compd no. | IC50 (μM) ± SEMa | ||||||
|---|---|---|---|---|---|---|---|
| MAO-A | MAO-B | SIb | eeAChE | eqBChE | SIb | Aβ1–42 peptide aggregation inhibition | |
| 18 | na | 10.043 ± 1.027 | — | 58.396 ± 0.09 | na | — | — |
| 19 | 89.546 ± 1.16 | 0.318 ± 0.021 | 281 | 15.241 ± 0.09 | 52.024 ± 1.422 | 3 | — |
| 20 | 10.028 ± 0.925 | 0.513 ± 0.070 | 19 | 13.510 ± 0.10 | 84.094 ± 1.318 | 6 | — |
| 21 | 37.118 ± 1.033 | 0.491 ± 0.024 | 75 | 29.837 ± 0.10 | 43.108 ± 1.09 | 1 | — |
| 22 | 19.403 ± 1.10 | 0.348 ± 0.041 | 55 | 0.172 ± 0.10 | 37.381 ± 1.17 | 217 | — |
| 23 | 10.011 ± 0.50 | 0.037 ± 0.011 | 270 | 0.071 ± 0.10 | 15.638 ± 0.901 | 220 | 23.11 ± 1.05 |
| 24 | 76.604 ± 1.225 | 0.142 ± 0.011 | 539 | 10.739 ± 0.10 | 58.217 ± 1.407 | 5 | — |
| 25 | 28.154 ± 1.093 | 0.066 ± 0.004 | 426 | 0.835 ± 0.10 | 14.130 ± 0.639 | 17 | 14.08 ± 0.24 |
| 26 | 19.881 ± 1.172 | 0.327 ± 0.011 | 60 | 0.890 ± 0.10 | 1.034 ± 0.031 | 1 | 19.52 ± 0.18 |
| 27 | na | 30.181 ± 1.183 | — | 49.033 ± 0.10 | na | — | — |
| 28 | 10.094 ± 0.239 | 0.219 ± 0.34 | 46 | 1.482 ± 0.10 | 9.251 ± 0.506 | 6 | 11.29 ± 0.08 |
| 29 | 21.428 ± 0.316 | 0.395 ± 0.34 | 54 | 3.642 ± 0.10 | 34.043 ± 1.18 | 9 | — |
| Safinamide | 8.204 ± 0.195 | 0.030 ± 0.001 | 273 | — | — | — | — |
| Donepezil | — | — | — | 0.055 ± 0.011 | 6.283 ± 0.026 | 114 | — |
| Curcumin | — | — | — | — | — | — | 7.29 ± 0.03 |
a
Values represent mean ± SEM; n = 3.
b
Selectivity index = SI = IC50 of MAO-A/IC50 of MAO-B and IC50 of BChE/IC50 of AChE; bold and italics boxes represents the compounds that have balanced (moderate to excellent) biological activities against all tested targets. na = no activity found in the tested concentration.