title: Potent and highly selective kappa opioid receptor agonists incorporating chroman- and 2,3-dihydrobenzofuran-based constraints.
abstract: Two novel chemical classes of kappa opioid receptor agonists, chroman-2-carboxamide derivatives and 2,3-dihydrobenzofuran-2-carboxamide derivatives, were synthesized. These agents exhibited high and selective affinity for the kappa opioid receptor.
authors.affiliation: Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA. ghchu@adolor.com
authors.forename: Guo-Hua
authors.initials: GH
authors.lastname: Chu
authors.forename: Minghua
authors.initials: M
authors.lastname: Gu
authors.forename: Joel A
authors.initials: JA
authors.lastname: Cassel
authors.forename: Serge
authors.initials: S
authors.lastname: Belanger
authors.forename: Thomas M
authors.initials: TM
authors.lastname: Graczyk
authors.forename: Robert N
authors.initials: RN
authors.lastname: DeHaven
authors.forename: Nathalie
authors.initials: N
authors.lastname: Conway-James
authors.forename: Mike
authors.initials: M
authors.lastname: Koblish
authors.forename: Patrick J
authors.initials: PJ
authors.lastname: Little
authors.forename: Diane L
authors.initials: DL
authors.lastname: DeHaven-Hudkins
authors.forename: Roland E
authors.initials: RE
authors.lastname: Dolle
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000701:Analgesics, Opioid / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D001572:Benzofurans / Q000737:chemistry; D002839:Chromans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D017473:Receptors, Opioid, kappa / Q000819:agonists*
chemical_list: D000577:Amides; D000701:Analgesics, Opioid; D001572:Benzofurans; D002839:Chromans; D017473:Receptors, Opioid, kappa; C043168:coumaran