Design and synthesis of novel cannabinoid ligands based on a 1,2,3- triazole scaffold
author:
Szafrański Przemysław , Dyduch Karol , Kościółek Tomasz, Wróbel Tomasz P. , Gomez-Canas Maria, Fernandez-Ruiz Javier, Młynarski Jacek , Gomes-Ruiz Maria
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.