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ID: ALA1132763

Journal: Bioorg Med Chem Lett

Title: 8-Aminocyclazocine analogues: synthesis and structure-activity relationships.

Authors: Wentland MP, Xu G, Cioffi CL, Ye Y, Duan W, Cohen DJ, Colasurdo AM, Bidlack JM.

Abstract: Opioid binding affinities were assessed for a series of cyclazocine analogues where the prototypic 8-OH substituent of cyclazocine was replaced by amino and substituted-amino groups. For mu and kappa opioid receptors, secondary amine derivatives having the (2R,6R,11R)-configuration had the highest affinity. Most targets were efficiently synthesized from the triflate of cyclazocine or its enantiomers using Pd-catalyzed amination procedures.

CiteXplore: 10673107

DOI: 10.1016/s0960-894x(99)00670-8