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Novel derivatives of 3-alkyl-1,5-diaryl-1H-1,2,4-triazoles and their pharmacological evaluation as CB1 cannabinoid ligands
Authors:Laura Hernandez-Folgado  Pilar Goya  Jordi Frigola  María Rosa Cuberes  Alberto Dordal  Jörg Holenz  Nadine Jagerovic
Affiliation:(1) Instituto de Química Médica (CSIC), Juan de la Cierva, Madrid, Spain;(2) Laboratorios del Dr. Esteve S. A., Barcelona, Spain
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 (CB1) receptor antagonists. However, the synthesis yields for the ligands were low. Here we present an alternative synthesis pathway with improved yields. In addition, we have synthezised new structural derivatives and studied their results in competitive radioligand binding assays for cannabinoid receptors. Correspondence: Nadine Jagerovic, Instituto de Química Médica (CSIC), Juan de la Cierva 3, E-28006-Madrid, Spain.
Keywords:Cannabinoid   1,2,4-Triazole   Binding.
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