Novel derivatives of 3-alkyl-1, 5-diaryl-1H-1, 2, 4-triazoles and their pharmacological evaluation as CB1 cannabinoid ligands

L Hernandez-Folgado, P Goya, J Frigola…

Index: Hernandez-Folgado, Laura; Goya, Pilar; Frigola, Jordi; Cuberes, Maria Rosa; Dordal, Alberto; Holenz, Joerg; Jagerovic, Nadine Monatshefte fur Chemie, 2008 , vol. 139, # 9 p. 1073 - 1082

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Abstract

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 (CB 1) 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.