Design and Synthesis of Novel Cannabinoid Ligands Based on a 1,2,3- triazole Scaffold
Following "click chemistry" guidelines, a 1,2,3-triazole scaffold was introduced in place of a benzene ring to mimic the non-classical cannabinoid pharmacophore model in a novel class of compounds aimed at CB1 receptor agonism. The design, synthesis and results of receptor
affinity tests for the new group of ligands are described. The obtained series exhibited a similar sidechainlength-activity relationship as in the initial pharmacophore model, with moderate CB1- selectivity.
Keywords: CB1 receptor; CP55940; Cannabinoid; Click chemistry; Non-classical cannabinoids; Triazole; column chromatography; cycloaddition; lipophilic side chain; pharmacophore model
Document Type: Research Article
Publication date: 01 February 2013
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