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  • Title: Discovery of piperidine carboxamide TRPV1 antagonists.
    Author: Cheung WS, Calvo RR, Tounge BA, Zhang SP, Stone DR, Brandt MR, Hutchinson T, Flores CM, Player MR.
    Journal: Bioorg Med Chem Lett; 2008 Aug 15; 18(16):4569-72. PubMed ID: 18662879.
    Abstract:
    A series of piperidine carboxamides were developed as potent antagonists of the transient receptor potential vanilloid-1 (TRPV1), an emerging target for the treatment of pain. A focused library of polar head groups led to the identification of a benzoxazinone amide that afforded good potency in cell-based assays. Synthesis and a QSAR model will be presented.
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