Synthesis and structure-activity relationships of a new series of 2α-substituted trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine as μ-selective opioid antagonists

Bertrand Le Bourdonnec, Allan J. Goodman, Mathieu Michaut, Hai Fen Ye, Thomas M. Graczyk, Serge Belanger, Robert N. DeHaven, Roland E. Dolle

Research output: Contribution to journalArticle

2 Scopus citations

Abstract

Structure-activity relationships at the 2α-position of the piperidine ring of the trans-4,5-dimethyl-4-(3-hydroxyphenyl)piperidine μ-opioid antagonist series were investigated. This study showed that only small linear alkyl groups (methyl, propyl) are tolerated at the 2α-position of the piperidine ring of this series.

Original languageEnglish
Pages (from-to)864-868
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume16
Issue number4
DOIs
StatePublished - Feb 15 2006
Externally publishedYes

Keywords

  • Antagonist
  • Opioid
  • μ

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