Table 7. CYP450 Isoform and MAO-A,B Inhibition Indices of in Vivo-Active Analogues 16, 18, 21, and 23.
CYP450 isoform, IC50 (μM) |
MAO inhibition (%) (30 μM
of each compound) |
|||||
---|---|---|---|---|---|---|
compd | 1A2 | 2C9 | 2D6 | 3A4 | A | B |
1 | >20 | >20 | >20 | >20 | 61.3 | 70.4 |
16 | >20 | >20 | >20 | >20 | 54.8 | 52.8 |
18 | >20 | >20 | >20 | >20 | 55.9 | 78.2 |
21 | >20 | >20 | >20 | 15 | 41.2 | 26.7 |
23 | >20 | >20 | >20 | >20 | 33.2 | 27.9 |