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. © 2017 Elsevier Ltd
Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as potential GABAA-R ligands / Gabriella, Guerrini; Ciciani, Giovanna; Daniele, Simona; lorenzo di cesare mannelli, ; Ghelardini, Carla; Martini, Claudia; Silvia, Selleri. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 25:(2017), pp. 1901-1906. [10.1016/j.bmc.2017.02.013]
Synthesis and pharmacological evaluation of pyrazolo[1,5-a]pyrimidin-7(4H)-one derivatives as potential GABAA-R ligands
GUERRINI, GABRIELLA;CICIANI, GIOVANNA;DI CESARE MANNELLI, LORENZO;GHELARDINI, CARLA;SELLERI, SILVIA
2017
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 10–30 mg/kg. © 2017 Elsevier Ltd
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