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
Letters in Drug Design & Discovery
Title:Design and Synthesis of Novel Cannabinoid Ligands Based on a 1,2,3- triazole Scaffold
Volume: 10 Issue: 2
Author(s): Przemyslaw W. Szafranski, Karol Dyduch, Tomasz Kosciolek, Tomasz P. Wrobel, Maria Gomez-Canas, Maria Gomez-Ruiz, Javier Fernandez-Ruiz and Jacek Mlynarski
Affiliation:
Keywords: Cannabinoid, CB1 receptor, Triazole, Click chemistry, Non-classical cannabinoids, pharmacophore model, cycloaddition, lipophilic side chain, column chromatography, CP55940
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.
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W. Szafranski Przemyslaw, Dyduch Karol, Kosciolek Tomasz, P. Wrobel Tomasz, Gomez-Canas Maria, Gomez-Ruiz Maria, Fernandez-Ruiz Javier and Mlynarski Jacek, Design and Synthesis of Novel Cannabinoid Ligands Based on a 1,2,3- triazole Scaffold, Letters in Drug Design & Discovery 2013; 10 (2) . https://dx.doi.org/10.2174/157018013804725134
DOI https://dx.doi.org/10.2174/157018013804725134 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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