Table 1.
In vitro COX-1 and COX-2 inhibitory IC50 values and COX SI values of the target compounds (5a-o).
| Compound ID | IC50 µM |
SIc COX-1/COX-2 |
|
|---|---|---|---|
| COX-1a | COX-2b | ||
| Celecoxib | 14.7 ± 0.06 | 0.05 ± 0.0003 | 294 |
| Rofecoxib | 14.5 ± 0.06 | 0.03 ± 0.0006 | 483.3 |
| Indomethacine | 0.1 ± 0.003 | 0.08 ± 0.0003 | 1.25 |
| Diclofenac sodium | 3.8 ± 0.03 | 0.84 ± 0.003 | 4.5 |
| 5a | 9.6 ± 0.06 | 0.11 ± 0.0003 | 87.3 |
| 5b | 12.2 ± 0.06 | 0.07 ± 0.0005 | 187.7 |
| 5c | 11.2 ± 0.08 | 0.08 ± 0.0003 | 145.5 |
| 5d | 10.6 ± 0.08 | 0.09 ± 0.001 | 116.5 |
| 5e | 8.3 ± 0.06 | 0.12 ± 0.003 | 69.2 |
| 5f | 9.7 ± 0.06 | 0.11 ± 0.003 | 88.2 |
| 5g | 10.5 ± 0.08 | 0.10 ± 0.0003 | 109.4 |
| 5h | 8.2 ± 0.12 | 0.14 ± 0.000 | 58.6 |
| 5i | 11.2 ± 0.11 | 0.08 ± 0.0008 | 136.6 |
| 5j | 12.2 ± 0.06 | 0.05 ± 0.0005 | 239.2 |
| 5k | 10.3 ± 0.08 | 0.09 ± 0.0003 | 111.9 |
| 5l | 10.2 ± 0.08 | 0.08 ± 0.001 | 134.2 |
| 5m | 9.9 ± 0.00 | 0.10 ± 0.0008 | 102.1 |
| 5n | 10.6 ± 0.08 | 0.07 ± 0.0005 | 153.6 |
| 5o | 12.9 ± 0.05 | 0.06 ± 0.0008 | 211.5 |
a,bConcentration of the compound that causes 50% inhibition of enzymatic activity of cyclooxygenase 1 and 2 (COX-1 and COX-2), respectively and all
values are expressed as Mean ± SEM of triplicate determinations.
cCOX-2 selectivity index: (COX-1 IC50/COX-2 IC50).