Table 2. P1 buried surface area/activity relationship.
The inhibitors have the generic formula of 9 except with a t-Boc cap instead of tert-butylurea.
| Compd | P1 | Ki* | SA | SA | Rel. Ki* SA | Rel. Ki* exp. | Ki* ratio exp./SA |
|---|---|---|---|---|---|---|---|
| 2 | Abu | 740 | 82 | 0 | 1 | 1 | 1.0 |
| 3 | Nva | 100 | 120 | 38 | 18 | 7 | 0.4 |
| 4 | Nle | 160 | 136 | 54 | 63 | 5 | 0.1 |
| 5 | c-Pra | 25 | 125 | 43 | 27 | 30 | 1.1 |
| 6 | c-Bua | 25 | 141 | 59 | 93 | 30 | 0.3 |