Table 5.
In vitro COX-1/COX-2 inhibition (IC50, μmol/L), selectivity index, ulcerogenic evaluation for compounds 75‒79, and standard agent.
| Compd. | COX-1a | COX-2a | COX-2 selectivityb | Ulcer index |
|---|---|---|---|---|
| 75 | 276.44 | 4.320 | 63.99 | 0.603 ± 0.15 |
| 76 | 76.67 | 25.87 | 2.963 | ‒ |
| 77 | 300.72 | 11.48 | 26.19 | 0.642 ± 0.25 |
| 78 | 33.58 | 7.750 | 4.332 | ‒ |
| 79 | 225.68 | 21.87 | 10.31 | 1.991 ± 0.34 |
| Celecoxib | >50 | 0.34 | 147.05 | 1.204 ± 0.06 |
a
The result (IC50, μmol/L) is the mean of three determinations acquired using a COX fluorescent inhibitor screening assay kit (Cayman Chemical, MI, USA).
b
COX-2 selectivity index (COX-1 IC50/COX-2 IC50).