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).

Autor: Le Bourdonnec B; Department of Chemistry, Adolor Corporation, Exton, Pennsylvania 19341, USA. blebourdonnec@adolor.com, Windh RT, Ajello CW, Leister LK, Gu M, Chu GH, Tuthill PA, Barker WM, Koblish M, Wiant DD, Graczyk TM, Belanger S, Cassel JA, Feschenko MS, Brogdon BL, Smith SA, Christ DD, Derelanko MJ, Kutz S, Little PJ, DeHaven RN, DeHaven-Hudkins DL, Dolle RE
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 2008 Oct 09; Vol. 51 (19), pp. 5893-6. Date of Electronic Publication: 2008 Sep 13.
DOI: 10.1021/jm8008986
Abstrakt: 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.
Databáze: MEDLINE