Table 7.
Functional and pharmacokinetic properties of oxy-substituted linker 13B analogsα
| Cpd | Structure | EC50 (nM) | hPPB (%) | mPPB (%) | t1/2 HLM (min) | t1/2 MLM (min) | PAMPA-BBB Pe (nm/sec) |
|---|---|---|---|---|---|---|---|
| 13B |  |
7.7 (5.40–10.74) | 90.4 | 96.7 | >145 | 127 | 22.9 |
| 23 |  |
9.63 (6.59–13.84) | 80.2 | 81.8 | >145 | >145 | 3.66 |
| 24 |  |
12.92 (8.56–18.81) | 57.1 | 60.4 | >145 | >145 | 1.176 |
| 25 |  |
3.31 (1.87–5.52) | 38.2 | 48.5 | >145 | >145 | 2.228 |
| 26 |  |
7.31 (3.33–23.51) | 55.2 | 66.4 | >145 | >145 | 23.799 |
| 27 |  |
6.28 (4.24–9.07) | 93.3 | 94.8 | 131.3 | 48.9 | 210.149 |
α
EC50 values are mean with 95% confidence limits.