3-Aryl pyridone derivatives. Potent and selective kappa opioid receptor agonists.
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.
Semple
Graeme
G
Department of Medicinal Chemistry, AstraZeneca R&D Mölndal, S-431 83, Mölndal, Sweden. graeme.semple@astrazeneca.com
Andersson
Britt-Marie
BM
Chhajlani
Vijay
V
Georgsson
Jennie
J
Johansson
Magnus
M
Lindschoten
Marcel
M
Pontén
Fritof
F
Rosenquist
Asa
A
Sörensen
Henrik
H
Swanson
Lars
L
Swanson
Marianne
M
D006801:Humans; D011485:Protein Binding; D011728:Pyridones / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D017473:Receptors, Opioid, kappa / Q000819:agonists* / Q000378:metabolism
D011728:Pyridones; D017473:Receptors, Opioid, kappa