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.
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.
Semple
Graeme
G
Department of Medicinal Chemistry, AstraZeneca R&D, Mölndal, S-431 83, Sweden. gsemple@arenapharm.com
Andersson
Britt Marie
BM
Chhajlani
Vijay
V
Georgsson
Jennie
J
Johansson
Magnus J
MJ
Rosenquist
Asa
A
Swanson
Lars
L
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
D007202:Indicators and Reagents; D019151:Peptide Library; D011728:Pyridones; D017465:Receptors, Opioid, delta; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D012996:Solutions