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- Title
Synthesis and Investigation of Anti-Inflammatory Activity of New Thiourea Derivatives of Naproxen.
- Authors
Nedeljković, Nikola; Dobričić, Vladimir; Bošković, Jelena; Vesović, Marina; Bradić, Jovana; Anđić, Marijana; Kočović, Aleksandar; Jeremić, Nevena; Novaković, Jovana; Jakovljević, Vladimir; Vujić, Zorica; Nikolić, Miloš
- 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.
- Subjects
ANTI-inflammatory agents; THIOUREA; NAPROXEN; AROMATIC amines; METHYL formate; AMINE derivatives
- Publication
Pharmaceuticals (14248247), 2023, Vol 16, Issue 5, p666
- ISSN
1424-8247
- Publication type
Article
- DOI
10.3390/ph16050666