Table 5. P4 buried surface area/activity relationship (generic formula 9, except P3= Chg rather than t-Bug).
Compd | P4 | Ki* | SA | Rel. Ki* SA | Rel. Ki* exp. | Ki* ratio exp./SA |
---|---|---|---|---|---|---|
14 | MeO(CO) | 800 | 0 | 1 | 1 | 1.0 |
15 | EtO(CO) | 230 | 22 | 5 | 3 | 0.6 |
16 | iPrO(CO) | 60 | 52 | 54 | 13 | 0.2 |
5 | tBuO(CO) | 25 | 52 | 54 | 32 | 0.6 |
17 | Ac-Val | 68 | 55 | 68 | 12 | 0.2 |