title: 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-1H-1,2,4-triazoles to be a novel class of cannabinoid type 1 receptor (CB1R) 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-1H-1,2,4-triazoles, and some of them were evaluated by CB1R radioligand binding assays. Compound 12a showed the most interesting pharmacological properties, possessing a CB1R affinity in the nanomolar range.
authors.affiliation: Instituto de Química Médica, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain.
authors.forename: Laura
authors.initials: L
authors.lastname: Hernandez-Folgado
authors.affiliation: Centros de Investigación en Red (CIBER) Fisiopatología de la Obesidad y Nutrición, Instituto de Salud Carlos III, CB06/03, 28029 Madrid, Spain; Unidad Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospitales Universitarios Regional y Virgen de la Victoria de Málaga, Universidad de Málaga, 29071 Málaga, Spain.
authors.forename: Juan
authors.initials: J
authors.lastname: Decara
authors.affiliation: Centros de Investigación en Red (CIBER) Fisiopatología de la Obesidad y Nutrición, Instituto de Salud Carlos III, CB06/03, 28029 Madrid, Spain; Unidad Gestión Clínica de Salud Mental, Instituto de Investigación Biomédica de Málaga (IBIMA), Hospitales Universitarios Regional y Virgen de la Victoria de Málaga, Universidad de Málaga, 29071 Málaga, Spain.
authors.forename: Fernando
authors.initials: F
authors.lastname: Rodríguez de Fonseca
authors.affiliation: Instituto de Química Médica, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain.
authors.forename: Pilar
authors.initials: P
authors.lastname: Goya
authors.affiliation: Instituto de Química Médica, CSIC, Juan de la Cierva 3, 28006 Madrid, Spain.
authors.forename: Nadine
authors.initials: N
authors.lastname: Jagerovic