Synthesis and evaluation of 3-amino-6-aryl-pyridazines as selective CB(2) agonists for the treatment of inflammatory pain.

Abstract

A series of 3-amino-6-aryl-pyridazines have been identified as CB(2) agonists with high efficacy and selectivity against the CB(1) receptor. Details of the investigation of structure-activity relationships (SAR) are disclosed, which led to the identification of pyridazine analogue 35, a compound with high potency in an in vivo model of inflammatory pain.

• Authors: Robert J Gleave, Paul J Beswick, Andrew J Brown, Gerard M P Giblin, Paul Goldsmith, Carl P Haslam, William L Mitchell, Neville H Nicholson, Lee W Page, Sadhana Patel, Susan Roomans, Brian P Slingsby, Martin E Swarbrick
• Journal: Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 20 Issue 2 Pg. 465-8 (Jan 15 2010) ISSN: 1464-3405 [Electronic] England
• PMID: 20005703 (Publication Type: Journal Article)
• Copyright: Copyright 2009 Elsevier Ltd. All rights reserved.

Chemical References

• Anti-Inflammatory Agents
• Isoquinolines
• Pyridazines
• Receptor, Cannabinoid, CB2

Topics

• Animals
• Anti-Inflammatory Agents (chemical synthesis, chemistry, pharmacokinetics)
• Isoquinolines (chemical synthesis, chemistry, pharmacokinetics)
• Pain (drug therapy)
• Pyridazines (chemical synthesis, chemistry, pharmacokinetics)
• Rats
• Receptor, Cannabinoid, CB2 (agonists, metabolism)
• Structure-Activity Relationship