【文章名】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)benzamid e (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)benzamid e (ADL5859).
作者
Le Bourdonnec, Bertrand;Windh, Rolf T.;Ajello, Christopher W.;Leister, Lara K.;Gu, Minghua;Chu, Guo-Hua;Tuthill, Paul A.;Barker, William M.;Koblish, Michael;Wiant, Daniel D.;Graczyk, Thomas M.;Belanger, Serge;Cassel, Joel A.;Feschenko, Marina S.;Brogdon,
[摘要]：Selective d opioid receptor agonists are promising potential therapeutic agents for the treatment of various types of pain conditions. A spirocyclic deriv. was identified as a promising hit through screening. Subsequent lead optimization identified compd. 20 (ADL5859) as a potent, selective, and orally bioavailable d agonist. Compd. 20 was selected as a clin. candidate for the treatment of pain.
