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3-Aryl pyridone derivatives. Potent and selective kappa opioid receptor agonists
Graeme Semple1, Britt-Marie Andersson, Vijay Chhajlani
1Department of Medicinal Chemistry, AstraZeneca R&D Mölndal, S-431 83, Mölndal, Sweden. graeme.semple@astrazeneca.com
Bioorganic & Medicinal Chemistry Letters
|January 5, 2002
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.