title: 3-Aryl pyridone derivatives. Potent and selective kappa opioid receptor agonists.
abstract: A new series of 3-aryl pyridone based kappa opioid receptor agonists was designed and synthesised, based on an understanding of the classical kappa opioid receptor pharmacophore. The most potent of the new compounds were comparable to U-69,593 in receptor affinity, selectivity and functional agonist effect at the cloned human kappa opioid receptor.
authors.affiliation: Department of Medicinal Chemistry, AstraZeneca R&D Mölndal, S-431 83, Mölndal, Sweden. graeme.semple@astrazeneca.com
authors.forename: Graeme
authors.initials: G
authors.lastname: Semple
authors.forename: Britt-Marie
authors.initials: BM
authors.lastname: Andersson
authors.forename: Vijay
authors.initials: V
authors.lastname: Chhajlani
authors.forename: Jennie
authors.initials: J
authors.lastname: Georgsson
authors.forename: Magnus
authors.initials: M
authors.lastname: Johansson
authors.forename: Marcel
authors.initials: M
authors.lastname: Lindschoten
authors.forename: Fritof
authors.initials: F
authors.lastname: Pontén
authors.forename: Asa
authors.initials: A
authors.lastname: Rosenquist
authors.forename: Henrik
authors.initials: H
authors.lastname: Sörensen
authors.forename: Lars
authors.initials: L
authors.lastname: Swanson
authors.forename: Marianne
authors.initials: M
authors.lastname: Swanson
mesh_terms: D006801:Humans; D011485:Protein Binding; D011728:Pyridones / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D017473:Receptors, Opioid, kappa / Q000819:agonists* / Q000378:metabolism
chemical_list: D011728:Pyridones; D017473:Receptors, Opioid, kappa