Potent, orally bioavailable delta opioid receptor agonists for the treatment of pain: Discovery of N,N-diethyl-4-(5-hydroxyspiro-[chromene-2, 4′-piperidine]-4-yl)benzamide (ADL5859)

Bertrand Le Bourdonnec, Rolf T. Windh, Christopher W. Ajello, Lara K. Leister, Minghua Gu, Guo Hua Chu, Paul A. Tuthill, William M. Barker, Michael Koblish, Daniel D. Wiant, Thomas M. Graczyk, Serge Belanger, Joel A. Cassel, Marina S. Feschenko, Bernice L. Brogdon, Steven A. Smith, David D. Christ, Michael J. Derelanko, Steve Kutz, Patrick J. LittleRobert N. DeHaven, Diane L. DeHaven-Hudkins, Roland E. Dolle

Research output: Contribution to journalArticlepeer-review

79 Scopus citations

Abstract

Selective δ opioid receptor agonists are promising potential therapeutic agents for the treatment of various types of pain conditions. A spirocyclic derivative was identified as a promising hit through screening. Subsequent lead optimization identified compound 20 (ADL5859) as a potent, selective, and orally bioavailable δ agonist. Compound 20 was selected as a clinical candidate for the treatment of pain.

Original languageEnglish
Pages (from-to)5893-5896
Number of pages4
JournalJournal of Medicinal Chemistry
Volume51
Issue number19
DOIs
StatePublished - Oct 9 2008

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