Institute of Natural Products Chemistry, Vietnam Academy of Science and Technology, 18 Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam,
Arch Pharm Res. 2013 Jul;36(7):832-9. doi: 10.1007/s12272-013-0100-z. Epub 2013 Apr 6.
A series of N-substituted-1,2,3-triazole murrayafoline A derivatives were successfully synthesized using click azide-alkyne Huisgen cycloaddition reaction between 1-methoxy-3-methyl-9-(3-azido)-propyl-9H-carbazole and substituted alkynes. Their chemical structures were confirmed by (1)H, (13)C NMR and HR-ESI-MS spectral data. In addition, the interested effects on LPS-stimulated production of pro-inflammatory cytokines in bone marrow-derived dendritic cells of synthetic murrayafoline A derivatives were also investigated. Our results indicated that murrayafoline A derivatives containing 1,2,3-triazole nucleus potentially possessed anti-inflammatory action through inhibiting production of IL-6, IL-12 p40 and TNF-α.
一系列 N-取代-1,2,3-三唑衍生物 Murrayafoline A 成功地通过点击叠氮化物-炔烃 Huisgen 环加成反应，由 1-甲氧基-3-甲基-9-(3-叠氮基)-丙基-9H-咔唑和取代的炔烃合成。其化学结构通过 (1)H、(13)C NMR 和 HR-ESI-MS 光谱数据得到证实。此外，还研究了合成的 Murrayafoline A 衍生物对 LPS 刺激的骨髓来源树突状细胞产生促炎细胞因子的影响。我们的结果表明，含有 1,2,3-三唑核的 Murrayafoline A 衍生物可能通过抑制 IL-6、IL-12 p40 和 TNF-α 的产生而具有抗炎作用。
