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Synthesis and Investigation of Anti-Inflammatory Activity of New Thiourea Derivatives of Naproxen
dc.creator | Nedeljković, Nikola | |
dc.creator | Dobričić, Vladimir | |
dc.creator | Bošković, Jelena | |
dc.creator | Vesović, Marina | |
dc.creator | Bradić, Jovana | |
dc.creator | Anđić, Marijana | |
dc.creator | Kočović, Aleksandar | |
dc.creator | Jeremić, Nevena | |
dc.creator | Novaković, Jovana | |
dc.creator | Jakovljević, Vladimir | |
dc.creator | Vujić, Zorica | |
dc.creator | Nikolić, Miloš | |
dc.date.accessioned | 2023-05-26T09:57:21Z | |
dc.date.available | 2023-05-26T09:57:21Z | |
dc.date.issued | 2023 | |
dc.identifier.issn | 1424-8247 | |
dc.identifier.uri | https://farfar.pharmacy.bg.ac.rs/handle/123456789/4756 | |
dc.description.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 | sr |
dc.language.iso | en | sr |
dc.publisher | MDPI | |
dc.relation | info:eu-repo/grantAgreement/ScienceFundRS/Ideje/7739840/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/inst-2020/200161/RS// | |
dc.relation | info:eu-repo/grantAgreement/MESTD/inst-2020/200111/RS// | |
dc.relation | Faculty of Medical Sciences, University of Kragujevac (Junior Project 11/20) | |
dc.rights | openAccess | sr |
dc.rights.uri | https://creativecommons.org/licenses/by/4.0/ | |
dc.source | Pharmaceuticals | sr |
dc.subject | naproxen; thiourea; carrageenan; paw edema; anti-inflammatory activity; COX-2; 5-LOX; molecular docking; FRED | sr |
dc.title | Synthesis and Investigation of Anti-Inflammatory Activity of New Thiourea Derivatives of Naproxen | sr |
dc.type | article | sr |
dc.rights.license | BY | sr |
dc.citation.volume | 16 | |
dc.citation.issue | 5 | |
dc.citation.rank | M21~ | |
dc.identifier.wos | 000997790100001 | |
dc.identifier.doi | 10.3390/ph16050666 | |
dc.identifier.pmid | 37242450 | |
dc.identifier.scopus | 2-s2.0-85160579060 | |
dc.identifier.fulltext | http://farfar.pharmacy.bg.ac.rs/bitstream/id/12994/Synthesis_and_Investigation_pub_2023.pdf | |
dc.type.version | publishedVersion | sr |