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

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

  • Bioorg Med Chem Lett. 2009 Jan 15;19(2):365-8. doi: 10.1016/j.bmcl.2008.11.076.
Mark P Wentland 1,  Qun Lu,  Rakesh Ganorkar,  Shao-Zhong Zhang,  Sunjin Jo,  Dana J Cohen,  Jean M Bidlack
Affiliations

Affiliation

  • 1 Department of Chemistry and Chemical Biology, Rensselaer Polytechnic Institute, 110 8th St., Troy, NY 12180, USA. [email protected]
PMID: 19091564 DOI: 10.1016/j.bmcl.2008.11.076
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.

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