Research Article
Synthesis, Biological Activity, and Molecular Modeling Studies of Pyrazole and Triazole Derivatives as Selective COX-2 Inhibitors
Table 1
In vitro activity on COX-1 and COX-2 with selectivity index.
| Compound | IC50 COX-1 (μM) | IC50 COX-2 (μM) | Selectivity index |
| 4a | 17.507 ± 1.050 | 1.386 ± 0.083 | 12.631 | 4b | 0.263 ± 0.016 | 0.017 ± 0.001 | 15.471 | 4c | 18.646 ± 1.119 | 1.305 ± 0.078 | 14.288 | 4d | 5.375 ± 0.323 | 0.098 ± 0.006 | 54.847 | 4e | 21.306 ± 1.278 | 0.551 ± 0.033 | 38.668 | 4f | 3.438 ± 0.206 | 1.902 ± 0.114 | 1.902 | 4g | 0.012 ± 0.001 | 1.460 ± 0.088 | 0.008 | 8a | 0.145 ± 0.009 | 3.324 ± 0.199 | 0.044 | 8b | 0.075 ± 0.005 | 0.226 ± 0.014 | 0.332 | 15a | 0.325 ± 0.020 | 0.002 ± 0.000 | 162.500 | 15b | 0.273 ± 0.016 | 0.131 ± 0.008 | 2.084 | Celecoxib | 1.479 ± 0.089 | 0.004 ± 0.000 | 369.750 |
|
|