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

Table 8. hMAO Enzyme Inhibition Activity of Donepezil–Picolinamide Hybrids.

6.

compound R n IC50 FOR MAO-A (μM) IC50 FOR MAO-B (μM) SI valuea
63 2-Br-Ph-CH2 2 NA 46.8 ± 2.2  
64 3-NO2–Ph 2 92.4 ± 7.1 26.2 ± 1.5 3.526
65 4-NO2–Ph 2 22.6 ± 1.8 68.3 ± 4 0.330
66 4-CH3–Ph 2 NA 94.1 ± 4.9  
67 4-Cl-Ph 2 23.2 ± 1.8 9.27 ± 1.3 2.502
68 2-quinoline 2 24.5 ± 2.3 48.6 ± 3.3 0.504
69 5-Cl-2-pyridine 2 13.4 ± 0.9 3.14 ± 0.27 4.267
70 6-CH3-2-pyridine 2 NA 2.53 ± 1.4  
71 5-Cl-2-thiophene 2 76.4 ± 5.4 11.5 ± 0.9 6.643
72 5-Br-2-thiophene 2 96.2 ± 4.8 9.47 ± 0.54 10.158
a

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