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

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.

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Main Authors: Peçanha,Emerson P., Fraga,Carlos A. M., Barreiro,Eliezer J., Braga,Maria F. M., Pereira,Edna F. R., Albuquerque,Edson X.
Format: Digital revista
Language:English
Published: Sociedade Brasileira de Química 2001
Online Access:http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532001000300013
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spelling oai:scielo:S0103-505320010003000132001-10-03Synthesis and pharmacological evaluation of a new 2-azabicyclo[3.3.0]octane derivativePeçanha,Emerson P.Fraga,Carlos A. M.Barreiro,Eliezer J.Braga,Maria F. M.Pereira,Edna F. R.Albuquerque,Edson X. 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.info:eu-repo/semantics/openAccessSociedade Brasileira de QuímicaJournal of the Brazilian Chemical Society v.12 n.3 20012001-06-01info:eu-repo/semantics/articletext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532001000300013en10.1590/S0103-50532001000300013
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language English
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author Peçanha,Emerson P.
Fraga,Carlos A. M.
Barreiro,Eliezer J.
Braga,Maria F. M.
Pereira,Edna F. R.
Albuquerque,Edson X.
spellingShingle Peçanha,Emerson P.
Fraga,Carlos A. M.
Barreiro,Eliezer J.
Braga,Maria F. M.
Pereira,Edna F. R.
Albuquerque,Edson X.
Synthesis and pharmacological evaluation of a new 2-azabicyclo[3.3.0]octane derivative
author_facet Peçanha,Emerson P.
Fraga,Carlos A. M.
Barreiro,Eliezer J.
Braga,Maria F. M.
Pereira,Edna F. R.
Albuquerque,Edson X.
author_sort Peçanha,Emerson P.
title Synthesis and pharmacological evaluation of a new 2-azabicyclo[3.3.0]octane derivative
title_short Synthesis and pharmacological evaluation of a new 2-azabicyclo[3.3.0]octane derivative
title_full Synthesis and pharmacological evaluation of a new 2-azabicyclo[3.3.0]octane derivative
title_fullStr Synthesis and pharmacological evaluation of a new 2-azabicyclo[3.3.0]octane derivative
title_full_unstemmed Synthesis and pharmacological evaluation of a new 2-azabicyclo[3.3.0]octane derivative
title_sort synthesis and pharmacological evaluation of a new 2-azabicyclo[3.3.0]octane derivative
description 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.
publisher Sociedade Brasileira de Química
publishDate 2001
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532001000300013
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