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

Members of a novel series of 7,8- and 8,9-fused triazole and imidazole analogues of cyclazocine display very high affinity for opioid receptors. 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 [ 35S]GTPγS...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2009-01, Vol.19 (2), p.365-368
Hauptverfasser: Wentland, Mark P., Lu, Qun, Ganorkar, Rakesh, Zhang, Shao-Zhong, Jo, Sunjin, Cohen, Dana J., Bidlack, Jean M.
Format: Artikel
Sprache:eng
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Zusammenfassung:Members of a novel series of 7,8- and 8,9-fused triazole and imidazole analogues of cyclazocine display very high affinity for opioid receptors. 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 [ 35S]GTPγS 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2008.11.076