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)

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• 作者：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 B
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：October 9, 2008
• 年：2008
• 卷：51
• 期：19
• 页码：5893-5896
• 全文大小：125K
• 年卷期：v.51,no.19(October 9, 2008)
• ISSN：1520-4804

文摘

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.