Table 11.
Inhibition constants and biodistribution of radioactivity of 2-arylimidazopyridine derivatives 140a–j (values are from [90]).
| Compound | R1 | R2 | R3 | Aβ1-40 Ki (nM) | %ID at 2 min | %ID at 60 min |
| 140a | H | H | NHMe | >1000 | — | — |
| 140b | H | H | NMe2 | >2000 | — | — |
| 140c | Me | H | NHMe | >2000 | — | — |
| 140d | Me | H | NMe2 | 242 ± 20 | — | — |
| 140e | I | H | NMe2 | 15 ± 5 | — | — |
| [125I]140e | 125I | H | NMe2 | — | 2.88 ± 0.25 | 0.21 ± 0.03 |
| 140f | Br | H | NMe2 | 10.3 ± 1.2 | — | — |
| 140g | Me | H | Br | 638 ± 30 | — | — |
| 140h | NMe2 | H | Br | 339 ± 40 | — | — |
| 140i | H | I | NMe2 | >2000 | — | — |
| 140j | I | I | NMe2 | >2000 | — | — |