Synthesis of novel cognition enhancers with pyrazolo[5,1-c][1,2,4]benzotriazine core acting at γ-aminobutyric acid type A (GABA(A)) receptor.

作者: Gabriella Guerrini , Giovanna Ciciani , Annarella Costanzo , Simona Daniele , Claudia Martini

DOI: 10.1016/J.BMC.2013.02.027

关键词:

摘要: Memory dysfunction associated with aging, neurodegenerative and psychiatric disorders represents an increasing medical need. Advances in research exploring the biological mechanisms underlying learning memory have opened new potential approaches for development of memory-enhancing therapies addressed to selective neuronal targets. In this work, we synthesized some derivatives a pyrazolo[5,1- c ][1,2,4]benzotriazine core identify ligands on GABA A receptors subtype (benzodiazepine site -receptor) endowed enhancing cognition activity without side effects usually non-selective modulators. fact, there is much evidence that -R (γ-aminobutyric acid, type receptor) relevance memory. vitro vivo tests been performed. Pharmacological data indicate compounds 7 , 13 14 22 act as dual functional modulators -Rs (promnemonic anxiolytic agents) while only 3 10 stand out selectively displaying good antiamnesic procognitive (1 3 mg/kg, respectively).

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