Table 3.
Compound | Pe (×106 cm/s)a | Predictionb |
---|---|---|
4a | 8.57 ± 1.23 | CNS+ |
4b | 8.78 ± 1.11 | CNS+ |
4c | 8.91 ± 2.03 | CNS+ |
4d | 8.82 ± 1.34 | CNS+ |
4e | 9.85 ± 0.98 | CNS+ |
4f | 6.30 ± 0.86 | CNS+ |
4g | 7.14 ± 1.97 | CNS+ |
4h | 6.42 ± 1.02 | CNS+ |
4i | 2.83 ± 0.65 | CNS± |
4j | 3.25 ± 0.82 | CNS± |
4k | 4.54 ± 0.84 | CNS+ |
4l | 7.35 ± 1.05 | CNS+ |
4m | 10.00 ± 2.63 | CNS+ |
9a | 8.79 ± 2.10 | CNS+ |
9b | 8.67 ± 1.76 | CNS+ |
aPermeability Pe (×106 cm/s) values are expressed as mean ± SD from three independent experiments, using PBS: EtOH (70:30) as solvent.
bCNS + is predicted as high BBB permeation with Pe (×106 cm/s) > 3.33, CNS ± is uncertain for BBB permeation with 1.51 < Pe (×106 cm/s) < 3.33.