Table 2.
SAR of southern amine substituent
| ||
|---|---|---|
| Cmp | R1 | IC50(μM)a |
| 1a |
|
0.46 |
| 1b |
|
0.56 |
| 1c |
|
2.0 |
| 1d |
|
0.22 |
| 1e |
|
2.4 |
| 1f |
|
6.4 |
| 1g |
|
9.9 |
| 1h |
|
4.9 |
| 1i |
|
9.2 |
| 1j |
|
>25 |
| 1k |
|
18 |
| 1l |
|
9.2 |
| 1m |
|
1.6 |
| 1n |
|
2.6 |
| 1o |
|
0.65 |
| 1p |
|
>25 |
| 1q |
|
0.89 |
| 1r |
|
1.3 |
Average of at least two measurements in DiI uptake assay with resynthesized or repurified compounds.