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

Publication date: Available online 11 February 2017
Source:Bioorganic & Medicinal Chemistry
Author(s): Guerrini Gabriella, Giovanna Ciciani, Simona Daniele, Lorenzo Di Cesare Mannelli, Carla Ghelardini, Claudia Martini, Silvia Selleri
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 10-30 mg/kg.

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