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  • Title: Developing piperine towards TRPV1 and GABAA receptor ligands--synthesis of piperine analogs via Heck-coupling of conjugated dienes.
    Author: Wimmer L, Schönbauer D, Pakfeifer P, Schöffmann A, Khom S, Hering S, Mihovilovic MD.
    Journal: Org Biomol Chem; 2015 Jan 28; 13(4):990-4. PubMed ID: 25438036.
    Abstract:
    Piperine, the pungent alkaloid of black pepper, and several of its derivatives are modulators of γ-amino butyric acid type A (GABAA) receptors. Concomitantly, this natural product has also been reported to activate transient receptor potential vanilloid type 1 (TRPV1) receptors. We have developed a Heck cross-coupling reaction of conjugated dienamides enabling the rapid assembly of piperine derivatives containing a modified aromatic core. Upon assessment of a focussed compound library, key aromatic substituents were identified selectively affecting either the GABAA or the TRPV1 receptor.
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