Article

Discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB2 agonists.

Department of Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA.
Bioorganic & medicinal chemistry letters (impact factor: 2.65). 08/2009; 19(17):5004-8. DOI:10.1016/j.bmcl.2009.07.057 pp.5004-8
Source: PubMed

ABSTRACT Recently sulfamoyl benzamides were identified as a novel series of cannabinoid receptor ligands. Replacing the sulfonamide functionality and reversing the original carboxamide bond led to the discovery of N-(3-(morpholinomethyl)-phenyl)-amides as potent and selective CB(2) agonists. Selective CB(2) agonist 31 (K(i)=2.7; CB(1)/CB(2)=190) displayed robust activity in a rodent model of postoperative pain.

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Keywords

cannabinoid receptor ligands
 
N-(3-(morpholinomethyl)-phenyl)-amides
 
novel series
 
original carboxamide bond
 
postoperative pain
 
sulfonamide functionality
 

Karin Worm