Author/Authors :
Mark P. Wentland، نويسنده , , Guoyou Xu، نويسنده , , Christopher L. Cioffi، نويسنده , , Yingchun Ye، نويسنده , , Wenhu Duan، نويسنده , , Dana J. Cohen، نويسنده , , Ann M. Colasurdo، نويسنده , , Jean M. Bidlack، نويسنده ,
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 μ and κ 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.
