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

摘要

In a previous study, we have identified 3-alkyl-l,5-charyl-lH-l,2,4-triazoles to be a novel class of cannabinoid type 1 receptor (CBXR) 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 l-benzyl-lH-l,2,4-triazoles, and some of them were evaluated by CBXR radioligand binding assays. Compound 12a showed the most interesting pharmacological properties, possessing a CBXR affinity in the nanomolar range.