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 |
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Hauptverfasser: | , , , , , , |
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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2008.11.076 |