Table 1.
Inhibition of PLA2 by 2-oxoamide esters. Average percent inhibition and standard error (n=3) reported for each compound at 0.091 mole fraction. N.D. signifies compounds with less than 25% inhibition (or no detectable inhibition).
| Entry | Structure | GIVA cPLA2 |
GVIA iPLA2 |
GV sPLA2 |
|---|---|---|---|---|
| 8a |  |
62 ± 1 | 45 ± 13 | 52 ± 4 |
| 8b |  |
74 ± 1 | 62 ± 13 | 62 ± 5 |
| 8c |  |
80 ± 2 | 53 ± 13 | 82 ± 8 |
| 8d |  |
N.D | N.D. | 48 ± 9 |
| 8e |  |
44 ± 2 | 51 ± 13 | 59 ± 8 |
| 8f |  |
79 ± 2 | 54 ± 13 | 72 ± 7 |
| 8g |  |
53 ± 2 | 63 ± 5 | 38 ± 8 |
| 8h |  |
35 ± 1 | N.D. | 58 ± 12 |
| 8i |  |
N.D. | N.D. | 42 ± 8 |
| 8j |  |
31 ± 2 | 35 ± 12 | 47 ± 6 |
| 8k |  |
74 ± 2 | 62 ± 13 | 72 ± 10 |