Benzyl-1,2,4-triazoles as CB 1 Cannabinoid Receptor Ligands: Preparation and In Vitro Pharmacological Evaluation

Abstract

In a previous study, we have identified 3-alkyl-1,5-diaryl-1 H -1,2,4-triazoles to be a novel class of cannabinoid type 1 receptor (CB 1 R) antagonists. In order to expand the number of cannabinoid ligands with a central 1,2,4-triazole scaffold, we have synthesized a novel series of 1-benzyl-1 H -1,2,4-triazoles, and some of them were evaluated by CB 1 R radioligand binding assays. Compound 12a showed the most interesting pharmacological properties, possessing a CB 1 R affinity in the nanomolar range.