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J Med Chem. 2008 Oct 9;51(19):5893-6. doi: 10.1021/jm8008986. Epub 2008 Sep 13.

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).

Author information

1
Department of Chemistry, Adolor Corporation, Exton, Pennsylvania 19341, USA. blebourdonnec@adolor.com

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.

PMID:
18788723
DOI:
10.1021/jm8008986
[Indexed for MEDLINE]

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