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ID: ALA3992560

Journal: Bioorg Med Chem

Title: Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as potential GABAA-R ligands.

Authors: Guerrini G, Ciciani G, Daniele S, Di Cesare Mannelli L, Ghelardini C, Martini C, Selleri S.

Abstract: The synthesis of a new series of 6-phenyl- and 6-benzylpyrazolo[1,5-a]pyrimidin-7(4H)-ones 2a-g and 3a-g, strictly related to derivatives with pyrazolobenzotriazine (PBT) and pyrazoloquinazoline (PQ) scaffold, was realized. The in vitro GABAA-receptor subtype affinity was evaluated and from preliminary pharmacological studies, compound 3g shows anxiolytic-like effect at 10-30mg/kg.

CiteXplore: 28237554

DOI: 10.1016/j.bmc.2017.02.013