Table 2. UUI and MIA of Compounds 1 and 2 in Scheme 1.
| UUIa |
|||||
|---|---|---|---|---|---|
| Compound | R1 | IC50 (μM) | % | MIAb IC50 (μM) or % | LogPc |
| 1 | 10.8 | 52.1 | 3.6 | 3.89 | |
| 2a | H | 2.5 | 67.5 | 43% | 2.70 |
| 2b | OMe | >100 | 21.7 | –10% | 2.57 |
| 2c | I | 5.3 | 65.1 | 53 μM | 4.05 |
| 2d | CN | 83.9 | 26.3 | 47% | 2.73 |
| 2e | SMe | >100 | 24.2 | 40 μM | 3.14 |
| 2f | tert-Butyl | 31.6 | 32.4 | 6.6 μM | 4.4 |
| 2g | Cyclopropyl | 8.8 | 67.8 | 24 μM | 3.43 |
| 2h | Cl | 14.7 | 38.2 | 31 μM | 3.26 |
| 2i | CF3 | >100 | 30.0 | 40% | 3.62 |