title: Synthesis and Biological activity of kappa opioid receptor agonists. Part 2: preparation of 3-aryl-2-pyridone analogues generated by solution- and solid-phase parallel synthesis methods.
abstract: New analogues of the previously described 3-aryl pyridone KOR agonists have been synthesised by parallel synthetic methods, both in solution- and with solid-phase chemistry, making use of the well known and versatile Mitsunobu, Suzuki and Buchwald reactions. Opioid receptor binding data for the compounds produced is reported.
authors.affiliation: Department of Medicinal Chemistry, AstraZeneca R&D, Mölndal, S-431 83, Sweden. gsemple@arenapharm.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 J
authors.initials: MJ
authors.lastname: Johansson
authors.forename: Asa
authors.initials: A
authors.lastname: Rosenquist
authors.forename: Lars
authors.initials: L
authors.lastname: Swanson
mesh_terms: D000478:Alkylation; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D007202:Indicators and Reagents; D019151:Peptide Library; D011728:Pyridones / Q000138:chemical synthesis* / Q000494:pharmacology*; D017465:Receptors, Opioid, delta / Q000737:chemistry / Q000378:metabolism; D017473:Receptors, Opioid, kappa / Q000819:agonists* / Q000737:chemistry; D017450:Receptors, Opioid, mu / Q000737:chemistry / Q000378:metabolism; D012996:Solutions; D013329:Structure-Activity Relationship
chemical_list: D007202:Indicators and Reagents; D019151:Peptide Library; D011728:Pyridones; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D012996:Solutions