2. Academic Validation
  3. 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)

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)

  • J Med Chem. 2008 Oct 9;51(19):5893-6. doi: 10.1021/jm8008986.
Bertrand Le Bourdonnec 1,  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 Little,  Robert N DeHaven,  Diane L DeHaven-Hudkins,  Roland E Dolle
Affiliations

Affiliation

  • 1 Department of Chemistry, Adolor Corporation, Exton, Pennsylvania 19341, USA. blebourdonnec@adolor.com
PMID: 18788723 DOI: 10.1021/jm8008986
Abstract

Selective delta 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 delta agonist. Compound 20 was selected as a clinical candidate for the treatment of pain.

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