Bioorganic and Medicinal Chemistry 2009-Jul
Synthesis of quinolinyl and isoquinolinyl phenyl ketones as novel agonists for the cannabinoid CB2 receptor.
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A series of quinolinyl and isoquinolinyl phenyl ketones was synthesized and their CB(2) receptor-dependent G-protein activities were determined using the [(35)S]GTPgammaS binding assay. Both quinoline and isoquinoline derivatives exhibited similar CB(2) receptor agonist activity, the most potent ligands being the 2-(Me(2)N)-phenyl substituted derivatives, which were also full agonists at the CB(2)-receptor.
