Table 3.
SAR of the anilide R2 group of the BZD compounds. Ki is the inhibition constant, the concentration of inhibitor that produces half-maximal inhibition.
| |||
|---|---|---|---|
| Compound | R2 | R3 | Ki (μM) |
| 8h |
|
|
> 200 |
| 9h |
|
|
> 200 |
| 8i |
|
|
147 ± 19 |
| 9i |
|
|
46 ± 7 |
| 8j |
|
|
62 ± 5 |
| 9j |
|
|
21 ± 2 |
| 8k |
|
|
89 ± 7 |
| 9k |
|
|
> 200 |
| 8l |
|
|
11 9 ± 40 |
| 9l |
|
|
> 200 |
| 8m |
|
|
> 200 |
| 9m |
|
|
> 200 |
| 8n |
|
|
95 ± 9 |
| 9n |
|
|
75 ± 7 |
| 8o |
|
|
> 200 |
| 9o |
|
|
11 ± 3 |
| 8p |
|
|
165 ± 11 |
| 9p |
|
|
11 ± 3 |
| 8q |
|
|
> 200 |
| 9q |
|
|
75 ± 7 |
| 8r |
|
|
143 ± 9 |
| 9r |
|
|
> 200 |
| 8s |
|
|
> 200 |
| 9s |
|
|
81 ± 28 |
| 8t |
|
|
> 200 |
| 9t |
|
|
49 ± 15 |