Table 5. In Vitro ADME Properties of Some Analoguesa.
| compound | Clint microsomes (μL/min/mg) mouse/human | solubility pH 6.8 (μg/mL) | PAMPA pH 7.4 (nm/s) |
|---|---|---|---|
| 7 | >500/112 | 59 | 441 |
| 12 | >500/95 | 15 | 291 |
| 47 | 154/<1 | 31 | 201 |
| 54 | ND | 83 | 258 |
| 55 | 24/7 | 84 | 219 |
| 64 | 452/188 | 69 | 364 |
| 67 | 318/205 | 0.1 | 416 |
| 70 | 464/150 | 10 | 408 |
| 80 | >500/NT | 0.7 | NT |
| 81 | >500/361 | 7.7 | 430 |
| 83 | >500/NT | NT | NT |
| 85 | 258/73 | 83 | 319 |
| 86 | ND | 90 | 219 |
| 87 | ND | 99 | 171 |
| 90 | 70/<1 | 94 | 220 |
ND: not determined, NT: not tested.