Design and Synthesis of Novel Cannabinoid Ligands Based on a 1,2,3- triazole Scaffold

Author(s): Przemyslaw W. Szafranski , Karol Dyduch , Tomasz Kosciolek , Tomasz P. Wrobel , Maria Gomez-Canas , Maria Gomez-Ruiz , Javier Fernandez-Ruiz , Jacek Mlynarski .

Journal Name: Letters in Drug Design & Discovery

Volume 10 , Issue 2 , 2013

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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: Cannabinoid, CB1 receptor, Triazole, Click chemistry, Non-classical cannabinoids, pharmacophore model, cycloaddition, lipophilic side chain, column chromatography, CP55940

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Article Details

Year: 2013
Page: [169 - 172]
Pages: 4
DOI: 10.2174/157018013804725134
Price: $58

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