Pronounced Anti‐Inflammatory and Analgesic Activities of a Spirofuran‐Triazolo[1,5‐a]pyrimidine Scaffold Available via Biginelli Multicomponent Condensation

In 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 ass...

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Veröffentlicht in:ChemistrySelect (Weinheim) 2024-09, Vol.9 (36), p.n/a
Hauptverfasser: Gümüş, Mustafa Kemal, Doğan, İnci Selin, Reis, Rengin, Sipahi, Hande, Uba, Abdullahi Ibrahim, Gorobets, Mykola Yu
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Sprache:eng
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Zusammenfassung:In 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 μM (p
ISSN:2365-6549
2365-6549
DOI:10.1002/slct.202402286