Table 2.
Inhibition of HIV-1 PR by BZDs alkylated at the anilide nitrogen with a 4-cyclohexylbenzyl moiety. Ki is the inhibition constant, the concentration of inhibitor that produces half-maximal inhibition.
| ||||
|---|---|---|---|---|
| Compound | R1 | R3 | R4 | Ki (μM) |
| 8a |
|
|
|
169 ± 27 |
| 9a |
|
|
|
85 ± 24 |
| 8b |
|
|
|
88 ± 6 |
| 9b |
|
|
|
56 ± 9 |
| 8c |
|
|
|
76 ± 7 |
| 9c |
|
|
|
27 ± 4 |
| 8d |
|
|
|
65 ± 12 |
| 9d |
|
|
|
19 ± 4 |
| 15 |
|
|
|
88 ± 5 |
| 16 |
|
|
|
68 ± 13 |
| 8e |
|
|
|
108 ± 12 |
| 9e |
|
|
|
53 ± 7 |
| 8f |
|
|
|
54 ± 7 |
| 9f |
|
|
|
47 ± 12 |
| 8g |
|
|
|
131 ± 8 |
| 9g |
|
|
|
72 ± 11 |