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, design...

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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: Article
Language:English
Published: Sociedade Brasileira de Química 2001-01-01
Series:Journal of the Brazilian Chemical Society
Subjects:
Online Access:http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532001000300013
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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.
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.
collection DOAJ
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.
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spelling doaj.art-96523a1a36cd4a289e92588a78a7f05a2022-12-21T17:00:53ZengSociedade Brasileira de QuímicaJournal of the Brazilian Chemical Society0103-50532001-01-01123408412Synthesis 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.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.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-505320010003000132-azabicyclo[3.3.0]octane derivativesdiastereoselective reductive-amination/cyclization one-pot processnebracetam analog
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
Journal of the Brazilian Chemical Society
2-azabicyclo[3.3.0]octane derivatives
diastereoselective reductive-amination/cyclization one-pot process
nebracetam analog
title 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_short 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
topic 2-azabicyclo[3.3.0]octane derivatives
diastereoselective reductive-amination/cyclization one-pot process
nebracetam analog
url http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532001000300013
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