Table 7.
In vitro COX-1/COX-2 inhibition (IC50, μmol/L), selectivity index, ulcerogenic evaluation (rat 50 mg/kg) and for compounds 87‒91, and standard agent.
| Compd. | COX-1a COX-2a | COX-2 selectivityb | Ulcer index | |
|---|---|---|---|---|
| 87 | >50 | 0.40 | >6.67 | 13.82 ± 0.62 |
| 88 | >50 | 0.52 | >96.15 | 11.56 ± 0.54 |
| 89 | >50 | 0.36 | >138.90 | 10.50 ± 0.63 |
| 90 | >50 | 0.46 | >108.70 | 11.75 ± 0.63 |
| 91 | >50 | 0.34 | >147.06 | 10.50 ± 0.59 |
| Celecoxib | >50 | 0.28 | >178.57 | 16.12 ± 0.86 |
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).