title: Novel malonamide derivatives as potent kappa opioid receptor agonists.
abstract: A novel series of malonamide derivatives was synthesized. These amides were shown to be potent and selective kappa opioid receptor agonists.
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: Michael
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: D002626:Chemistry, Pharmaceutical / Q000379:methods*; D019389:Cytochrome P-450 CYP2D6 / Q000737:chemistry; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D020128:Inhibitory Concentration 50; D007700:Kinetics; D008314:Malonates / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D008956:Models, Chemical; D008968:Molecular Conformation; D017473:Receptors, Opioid, kappa / Q000037:antagonists & inhibitors*
chemical_list: D008314:Malonates; D017473:Receptors, Opioid, kappa; D019389:Cytochrome P-450 CYP2D6; C008314:malonamide