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. 2023 Oct 3;8(41):37731–37751. doi: 10.1021/acsomega.3c05883

Table 6. hMAO Enzyme Inhibitory Activity of Donepezil–ASS234 Hybrids.

4.

compound n R1 R2 IC50 for MAO-A (μM) IC50 for MAO-B (μM) SI valuea
40 0 –Ph –Me >100 >100 1
41 1 –Ph –Me >100 >100 1
42 2 –Ph –Me >100 >100 1
43 3 –Ph –Me >100 >100 1
44 0 –Ph –H 14.1 ± 3.8 >100 0.141
45 2 –H –Me >100 >100 1
46 0 –H –H >100 >100 1
47 2 –H –H >100 >100 1
48 4 –Ph –Me 5.7 ± 2.1 >100 0.057
49 2 –Ph –H >100 >100 1
50 3 –Ph –H >100 >100 1
51 4 –Ph –H >100 >100 1
52 3 –H –Me >100 6.11 ± 1.4 16.366
53 4 –H –Me >100 3.95 ± 0.94 25.316
54 3 –H –H >100 >100 1
55 4 –H –H >50 >50 1
a

Selectivity index for MAO-B (IC50 for MAO-A/IC50 for MAO-B).