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Letters in Drug Design & Discovery

Editor-in-Chief

ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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 and Jacek Mlynarski

Volume 10, Issue 2, 2013

Page: [169 - 172] Pages: 4

DOI: 10.2174/157018013804725134

Price: $65

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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