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8-Aminocyclazocine analogues: synthesis and structure–activity relationships

✍ Scribed by Mark P Wentland; Guoyou Xu; Christopher L Cioffi; Yingchun Ye; Wenhu Duan; Dana J Cohen; Ann M Colasurdo; Jean M Bidlack

Publisher
Elsevier Science
Year
2000
Tongue
English
Weight
166 KB
Volume
10
Category
Article
ISSN
0960-894X

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✦ Synopsis

AbstractÐOpioid binding anities 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 m and k opioid receptors, secondary amine derivatives having the (2R,6R,11R)-con®guration had the highest anity. Most targets were eciently synthesized from the tri¯ate of cyclazocine or its enantiomers using Pd-catalyzed amination procedures.

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