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  • Title: Novel unsaturated glycyrrhetic acids derivatives: Design, synthesis and anti-inflammatory activity.
    Author: Li B, Cai S, Yang YA, Chen SC, Chen R, Shi JB, Liu XH, Tang WJ.
    Journal: Eur J Med Chem; 2017 Oct 20; 139():337-348. PubMed ID: 28803048.
    Abstract:
    To develop novel anti-inflammatory agents, a series of unsaturated glycyrrhetic acids were designed, synthesized and evaluated for anti-inflammatory activity using RAW264.7 cells. The structure-activity relationship (SAR) of NO inhibitory activity was analyzed. α,β-Unsaturated glycyrrhetic acids showed better activity, among them, compounds 6k and 6l with piperazine unit exhibited the most potent nitric oxide (NO) and interleukin-6 (IL-6) inhibitory activity (IC50 = 13.3 and 15.5 μM respectively). Furthermore, compound 6k could also significantly suppress LPS-induced iNOS and COX-2 expression and IL-6 production through MAPKs and NF-kB signaling pathway.
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