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Development of novel tail-modified anandamide analogs

Development of novel tail-modified anandamide analogs

  1. ThirdEyeFloond
    Bioorganic & Medicinal Chemistry Letters
    Volume 18, Issue 22, 15 November 2008, Pages 5912-5915

    Fenmei Yao, Chen Li, Subramanian K. Vadivel, Anna L. Bowman and Alexandros Makriyannis

    Abstract

    To explore the hydrophobic groove subsite within the CB1 cannabinoid receptor we have designed and synthesized a group of tail-substituted anandamide analogs. Our design involves the introduction of aryl or heterocyclic ring as terminal substituents that are connected to the last cis-arachidonyl double bond through aliphatic chains of variable lengths. Our results indicate that there are strict stereochemical requirements for the interaction of such analogs with the CB1 receptor. The optimal pharmacophore includes the phenyl, p-substituted phenyl, or 3-furyl substituents attached to the cis-double bond through a four methylene chain.
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