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The aim of the study was a synthesis and investigation of the dose-dependent anti-inflammatory effect of new thiourea derivatives of naproxen with selected aromatic amines and esters of aromatic amino acids. The results of the in vivo study indicate that derivatives of <i>m</i>-anisidine (<b>4</b>) and <i>N</i>-methyl tryptophan methyl ester (<b>7</b>) showed the most potent anti-inflammatory activity four hours after injection of carrageenan, with the percentage of inhibition of 54.01% and 54.12%, respectively. In vitro assays of COX-2 inhibition demonstrated that none of the tested compounds achieved 50% inhibition at concentrations lower than 100 µM. On the other hand, the aromatic amine derivatives (<b>1</b>–<b>5</b>) accomplished significant inhibition of 5-LOX, and the lowest IC₅₀ value was observed for compound <b>4</b> (0.30 μM). High anti-edematous activity of compound <b>4</b> in the rat paw edema model, together with potent inhibition of 5-LOX, highlight this compound as a promising anti-inflammatory agent.