Table 2.
In vitro COX-1/COX-2 inhibition (IC50, μmol/L), selectivity index, ulcerogenic evaluation for compounds 18–21, and standard agents.
| Compd. | COX-1a COX-2a | COX-2 selectivityb | Ulcer index | |
|---|---|---|---|---|
| 18 | 4.52 | 0.42 | 10.76 | 1.22 |
| 19 | 6.74 | 0.62 | 10.87 | 3.02 |
| 20 | 4.52 | 0.52 | 8.69 | 2.60 |
| 21 | 7.86 | 0.86 | 9.14 | 2.61 |
| Celecoxib | 7.23 | 0.84 | 8.61 | 2.93 |
| Ibuprofen | ‒ | ‒ | ‒ | 20.25 |
The result (IC50, μmol/L) is the mean of three determinations acquired using a COX fluorescent inhibitor screening assay kit (Cayman Chemical, MI, USA).
COX-2 selectivity index (COX-1 IC50/COX-2 IC50).