Table 12. hMAO Inhibition Property of Donepezil–Butylated Hydroxytoluene (BHT) Hybrids.
compound | R | IC50 for MAO-A (μM) | IC50 for MAO-B (μM) | SI valuea |
---|---|---|---|---|
139 | H | 62.3 ± 3.1 | 8.5 ± 0.3 | 7.329 |
140 | 4-OCH3 | 72.5 ± 5.1 | 6.7 ± 1.2 | 10.820 |
141 | 2-CH3 | 69.3 ± 3.2 | 7.2 ± 0.2 | 9.625 |
142 | 3-CH3 | 70.1 ± 0.1 | 8.9 ± 0.3 | 7.876 |
143 | 2-F | 60.2 ± 0.4 | 7.4 ± 0.2 | 8.135 |
144 | 3-F | 58.4 ± 0.5 | 6.5 ± 0.2 | 8.984 |
145 | 4-F | 59.6 ± 0.4 | 11.1 ± 0.1 | 5.369 |
146 | 2,4–2F | 70.6 ± 0.3 | 12.5 ± 1.1 | 5.648 |
147 | 3,4–2F | 64.5 ± 1.2 | 9.3 ± 0.2 | 6.935 |
148 | 2-Cl | 72.1 ± 2.2 | 9.8 ± 0.2 | 7.357 |
149 | 3-Cl | 65.1 ± 2.3 | 8.7 ± 0.1 | 7.482 |
150 | 4-Br | 73.2 ± 1.1 | 13.2 ± 1.2 | 5.545 |
151 | 3-NO2 | 70.9 ± 1.4 | 12.5 ± 1.1 | 5.672 |
152 | 4-CN | 78.2 ± 1.3 | 13.9 ± 0.3 | 5.625 |
Selectivity index for MAO-B (IC50 for MAO-A/IC50 for MAO-B).