Table 2.
Modification of the benzyl amide of 1.
 | |||
|---|---|---|---|
| No | R | IC50 (μM)a | CC50 (μM)b |
| 125 |  |
15.6 ±1.8 | >100 |
| 5c |  |
30.6 ± 7.3 | >100 |
| 6 |  |
>100 | >100 |
| 7 |  |
>100 | >100 |
| 8 |  |
>100 | >100 |
| 9 |  |
>100 | >100 |
| 10 |  |
>100 | >100 |
| 11 |  |
>100 | >100 |
| 12 |  |
0.53 ±0.04 | >100 |
| 13 |  |
1.7 ± 0.1 | >100 |
| 14 |  |
7.1 ± 0.9 | >100 |
| 1525 |  |
15.2 ± 4.7 | 62 ± 13 |
| 16 |  |
>100 | >50 |
a
Inhibition of luciferase expression in WEEV replicon assay.
b
Cell viability determined by the MTT reduction assay. Values are mean of at least n=3 independent experiments.
c
Based on nipecotic acid central ring (racemate).25