Effect of anchoring 4-anilidopiperidines to opioid peptides

Ravil R. Petrov, Yeon Sun Lee, Ruben S. Vardanyan, Lu Liu, Shou Wu Ma, Peg Davis, Josephine Lai, Frank Porreca, Todd W. Vanderah, Victor J. Hruby

Research output: Contribution to journalArticle

7 Scopus citations

Abstract

We report here the design, synthesis, and in vitro characterization of new opioid peptides featuring a 4-anilidopiperidine moiety. Despite the fact that the chemical structures of fentanyl surrogates have been found suboptimal per se for the opioid activity, the corresponding conjugates with opioid peptides displayed potent opioid activity. These studies shed an instructive light on the strategies and potential therapeutic values of anchoring the 4-anilidopiperidine scaffold to different classes of opioid peptides.

Original languageEnglish (US)
Pages (from-to)3434-3437
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number11
DOIs
StatePublished - Jun 1 2013

Keywords

  • Analgesic
  • Bivalent ligand
  • Dynorphine analog
  • Fentanyl
  • Opioid peptide

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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