Table 1.
In-vitro COX-1 and COX-2 enzyme inhibition assay data for 4-(Imidazolylmethyl)-2-(4- methylsulfony phenyl)-Quinolinederivatives(9a-9e).
| Compound | R 1 | R 2 | COX-1 IC 50 a (µM) | COX-2 IC 50 a (µM) | Selectivity Index b |
|---|---|---|---|---|---|
| 9d | Cyclohexyl | 34.5 | 0.063 | 547.6 | |
| 9c | Phenyl | 35.9 | 0.068 | 527.9 | |
| 9a | Phenyl | H | 30.1 | 0.071 | 423.9 |
| 9b | Me | Me | 26.0 | 0.090 | 288.9 |
| 9e | H | H | 12.95 | 0.072 | 179.9 |
| Celecoxib | 24.3 | 0.060 | 405 | ||
a
Values are means of two determinations acquired using an ovine COX-1/COX-2 assay kit and the deviation from the mean is < 10% of the mean value.
b
In-vitro COX-2 selectivity index (COX-1 IC50/COX-2 IC50).