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Synthesis and Investigation of Anti-Inflammatory Activity of New Thiourea Derivatives of Naproxen.

ABSTRACT: 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 m-anisidine (4) and N-methyl tryptophan methyl ester (7) 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 (1-5) accomplished significant inhibition of 5-LOX, and the lowest IC50 value was observed for compound 4 (0.30 μM). High anti-edematous activity of compound 4 in the rat paw edema model, together with potent inhibition of 5-LOX, highlight this compound as a promising anti-inflammatory agent.

SUBMITTER: Nedeljkovic N 

PROVIDER: S-EPMC10222328 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature

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Synthesis and Investigation of Anti-Inflammatory Activity of New Thiourea Derivatives of Naproxen.

Nedeljković Nikola N   Dobričić Vladimir V   Bošković Jelena J   Vesović Marina M   Bradić Jovana J   Anđić Marijana M   Kočović Aleksandar A   Jeremić Nevena N   Novaković Jovana J   Jakovljević Vladimir V   Vujić Zorica Z   Nikolić Miloš M  

Pharmaceuticals (Basel, Switzerland) 20230428 5

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 54.1  ...[more]

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