, 2024.
A dual COX/5-LOX strategy was adopted to develop new oxindole derivatives with superior anti-inflammatory activity. Three series of oxindoles - esters -, - and imines - - were synthesized and evaluated for their anti-inflammatory and analgesic activities. Molecular docking and predicted pharmacokinetic parameters were done for the most active compounds. A new LC-MS/MS method was developed and validated for the quantification of in rat plasma. Compounds , , , and revealed % edema inhibition up to 100.00%; also, and showed 100.00% writhing protection. Compound showed dual inhibitory activity with IC = 0.0533 and 0.4195 μM for COX-2 and 5-LOX, respectively. Molecular docking rationalized the obtained biological activity. The pharmacokinetic parameters of from rat plasma were obtained.