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

• Հիմնական հեղինակներ: Nikola Nedeljković (Հեղինակ), Vladimir Dobričić (Հեղինակ), Jelena Bošković (Հեղինակ), Marina Vesović (Հեղինակ), Jovana Bradić (Հեղինակ), Marijana Anđić (Հեղինակ), Aleksandar Kočović (Հեղինակ), Nevena Jeremić (Հեղինակ), Jovana Novaković (Հեղինակ), Vladimir Jakovljević (Հեղինակ), Zorica Vujić (Հեղինակ), Miloš Nikolić (Հեղինակ)
• Ձևաչափ: Գիրք
• Հրապարակվել է: MDPI AG, 2023-04-01T00:00:00Z.
• Խորագրեր: article
• Առցանց հասանելիություն: Connect to this object online.

Ամփոփում

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.

Նյութի նկարագրություն

10.3390/ph16050666
1424-8247