Synthesis and pharmacological evaluation of a new 2-azabicyclo[3.3.0]octane derivative

• Autor(a) principal: Peçanha,Emerson P.
• Data de Publicação: 2001
• Outros Autores: Fraga,Carlos A. M., Barreiro,Eliezer J., Braga,Maria F. M., Pereira,Edna F. R., Albuquerque,Edson X.
• Tipo de documento: Artigo
• Idioma: eng
• Título da fonte: Journal of the Brazilian Chemical Society (Online)
• Texto Completo: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532001000300013
• topic: 2-azabicyclo[3.3.0]octane derivatives; diastereoselective reductive-amination/cyclization one-pot process; nebracetam analog

As part of a research program aiming at the design, synthesis and pharmacological evaluation of a novel lead-candidates of neuroactive compounds, we describe herein the synthesis and the central profile of a new nebracetam analog having a 2-aza-bicyclo[3.3.0]octane system. The new derivative, designed on the basis of the conformational restriction concept, was synthesized in good yields exploring a diastereoselective reductive-amination and cyclization one-pot sequence. The pharmacological profile of this new compound, investigated by using path-clamp techniques on neurons of the CNS, indicated no effects on these cells.