A new class of pyrazolo[5,1-c][1,2,4]triazines as γ-aminobutyric type A (GABAA) receptor subtype ligand: synthesis and pharmacological evaluation

Publication date: Available online 4 April 2018
Source:Bioorganic & Medicinal Chemistry
Author(s): Gabriella Guerrini, Giovanna Ciciani, Simona Daniele, Claudia Martini, Camilla Costagli, Chiara Guarino, Silvia Selleri
A comparison between compounds with pyrazolo[1,5-a]pyrimidine structure (series 4-6) and pyrazolo[5,1-c][1,2,4]triazine core (series 9) as ligands at GABAA-receptor subtype, was evaluated. Moreover, for pyrazolotriazines derivatives having binding recognition, the interaction on recombinant rat α (1-3,5) GABAA receptor subtypes, was performed. Among these latter, emerge compounds 9c, 9k, 9l, 9m and 9n as α 1-selective and 9h as α 2-selective ligands.

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