1. Academic Validation
  2. 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

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

  • Bioorg Med Chem Lett. 2003 Mar 24;13(6):1141-5. doi: 10.1016/s0960-894x(03)00033-7.
Graeme Semple 1 Britt Marie Andersson Vijay Chhajlani Jennie Georgsson Magnus J Johansson Asa Rosenquist Lars Swanson
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, AstraZeneca R&D, Mölndal, S-431 83, Sweden. gsemple@arenapharm.com
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.

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