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

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