Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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.

Abstract:

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

VOLUME: 10
ISSUE: 2
Year: 2013
Page: [169 - 172]
Pages: 4
DOI: 10.2174/157018013804725134
Price: $58