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    Bioorg Med Chem Lett. 2009 Jan 15;19(2):365-8. Epub 2008 Nov 24.

    Redefining the structure-activity relationships of 2,6-methano-3-benzazocines. Part 7: syntheses and opioid receptor properties of cyclic variants of cyclazocine.

    Wentland MP, Lu Q, Ganorkar R, Zhang SZ, Jo S, Cohen DJ, Bidlack JM.

    Source

    Department of Chemistry and Chemical Biology, Rensselaer Polytechnic Institute, 110 8th St., Troy, NY 12180, USA. wentmp@rpi.edu

    Abstract

    A series of 7,8- and 8,9-fused triazole and imidazole analogues of cyclazocine have been made and characterized in opioid receptor binding and [(35)S]GTPgammaS assays. Target compounds were designed to explore the SAR surrounding our lead molecule for this study, namely the 8,9-fused pyrrolo analogue 2 of cyclazocine. Compared to 2, many of the new compounds in this study displayed very high affinity for opioid receptors.

    PMID:
    19091564
    [PubMed - indexed for MEDLINE]

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