期刊
FUTURE MEDICINAL CHEMISTRY
卷 12, 期 1, 页码 5-17出版社
FUTURE SCI LTD
DOI: 10.4155/fmc-2019-0234
关键词
ERK1/2 pathway; green chemistry; indoles; inflammation; Mannich reaction; multicomponent reaction; NF-kappa B pathway
Aim: Over the years, indole has proved to be a versatile scaffold for the design of molecules acting as anti-inflammatory agents. Materials & Methods: A small library of 3-amino-alkylated indoles has been obtained by an optimized Mannich green approach. The anti-inflammatory activity of the new 3-amino-alkylated indoles, GLYC 0-10, was evaluated in RAW 264.7 macrophages. Results: The anti-inflammatory activity of the new 3-amino-alkylated indoles, GLYC 0-10, was evaluatedn and, among them, GLYC 4, 5 and 9 displayed the greatest inhibitory effects on nitric oxide production, with IC50 values of 5.41, 4.22 and 6.3 mu M, respectively. Conclusion: Our outcomes, overall, highlight the importance of the indole substitution in the anti-inflammatory activity of these compounds, exerted by acting on the interlinked NF-kappa B/ERK1/2 pathways. [GRAPHICS] .
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