Pronounced anti-inflammatory and analgesic activities of a spirofuran-triazolo[1,5-a]pyrimidine scaffold available via biginelli multicomponent condensation

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dc.contributor.authorGümüş, Mustafa Kemal
dc.contributor.authorDoğan, İnci Selin
dc.contributor.authorReis, Rengin
dc.contributor.authorSipahi, Hande
dc.contributor.authorUba, Abdullahi Ibrahim
dc.contributor.authorGorobets, Mykola Yu
dc.date.accessioned2024-11-25T11:09:16Z
dc.date.available2024-11-25T11:09:16Z
dc.date.issued2024
dc.departmentAÇÜ, Artvin Meslek Yüksekokulu, Laboratuvar Teknolojisi Bölümüen_US
dc.description.abstractIn this work, a series of phenyl-derivatives of spirofuran-triazolo[1,5-a]pyrimidine (5 a–i) were evaluated for their anti-inflammatory and analgesic activities, including SAR and molecular docking studies. The cytotoxicity of compounds was studied in RAW 264.7 murine macrophage cell line by MTT assay. Then, those with cell viability higher than 70 % were tested for their anti-inflammatory activity at their non-toxic doses by evaluating the nitrite level of the cell supernatants with the Griess reagent. Compounds 5 b, 5 d, 5 e, and 5 g demonstrated significant inhibition of nitrite production by 49 %, 59 %, 63 % respectively at 100 ?M (p<0.05), whereas 56 % inhibition was seen with 50 ?M of 5 g. According to the inhibition of PGE2, compound 5 b showed the most notable effect compared to control. All tested compounds, particularly 5 b, 5 d, 5 e and 5 f reduced the PGE? level and showed potential analgesic activity. Seven heterocycles 5 a–g showed moderate to significant anti-inflammatory and analgesic activities. Molecular docking predicts modest or no inhibition of 5 a–i with COX-1. Instead, the modelling results also show that these molecules can effectively bind to the enzymes COX-2 and mPGES-2. However, the simulation distinguished the key role of the 2-OH group in stabilizing the inhibitor-target complex only in the case of binding to COX-2.
dc.identifier.doi10.1002/slct.202402286
dc.identifier.issn2365-6549
dc.identifier.issue36en_US
dc.identifier.scopusqualityQ3
dc.identifier.urihttp://dx.doi.org/10.1002/slct.202402286
dc.identifier.urihttps://hdl.handle.net/11494/5006
dc.identifier.volume9en_US
dc.identifier.wosqualityQ3
dc.indekslendigikaynakWeb of Science
dc.indekslendigikaynakScopus
dc.language.isoenen_US
dc.publisherJohn Wiley and Sons Incen_US
dc.relation.ispartofChemistrySelect
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.rightsinfo:eu-repo/semantics/embargoedAccessen_US
dc.subjectAnti-Inflammatory Activityen_US
dc.subjectBiginelli Reactionen_US
dc.subjectMolecular Dockingen_US
dc.subjectMTT Assayen_US
dc.subjectPGE₂en_US
dc.titlePronounced anti-inflammatory and analgesic activities of a spirofuran-triazolo[1,5-a]pyrimidine scaffold available via biginelli multicomponent condensationen_US
dc.typeArticle

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