A química medicinal de N-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticos

Detalhes bibliográficos
Autor(a) principal: Barreiro,Eliezer J.
Data de Publicação: 2002
Outros Autores: Fraga,Carlos A. M., Miranda,Ana L. P., Rodrigues,Carlos R.
Tipo de documento: Artigo
Idioma: por
Título da fonte: Química Nova (Online)
Texto Completo: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-40422002000100022
Resumo: In this article are described new bioactive N-acylhydrazone (NAH) derivatives, structurally designed as optimization of aryl hydrazones precursors planned by molecular hybridization of two 5-lipoxigenase inhibitors, e.g. CBS-1108 and BW-755c. The analgesic, antiedematogenic and anti-platelet aggregating profile of several isosteric compounds was investigated by using classic pharmacological assays in vivo and ex-vivo, allowing to identify new potent peripheric analgesic lead, a new anti-inflammatory and an antithrombotic agent. During this study was discovered dozen of active NAH compounds clarifying the structure-activity relationship for this series of NAH derivatives, indicating the pharmacophore character of the N-acylhydrazone functionality.
id SBQ-3_5bc5a4adf5a08f9153a9484342e63296
oai_identifier_str oai:scielo:S0100-40422002000100022
network_acronym_str SBQ-3
network_name_str Química Nova (Online)
repository_id_str
spelling A química medicinal de N-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticosbioactive N-acylhydrazones derivativesantiinflammatory, analgesic and antithrombotic propertiesmolecular hybridization and bioisosterism in drug designIn this article are described new bioactive N-acylhydrazone (NAH) derivatives, structurally designed as optimization of aryl hydrazones precursors planned by molecular hybridization of two 5-lipoxigenase inhibitors, e.g. CBS-1108 and BW-755c. The analgesic, antiedematogenic and anti-platelet aggregating profile of several isosteric compounds was investigated by using classic pharmacological assays in vivo and ex-vivo, allowing to identify new potent peripheric analgesic lead, a new anti-inflammatory and an antithrombotic agent. During this study was discovered dozen of active NAH compounds clarifying the structure-activity relationship for this series of NAH derivatives, indicating the pharmacophore character of the N-acylhydrazone functionality.Sociedade Brasileira de Química2002-02-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-40422002000100022Química Nova v.25 n.1 2002reponame:Química Nova (Online)instname:Sociedade Brasileira de Química (SBQ)instacron:SBQ10.1590/S0100-40422002000100022info:eu-repo/semantics/openAccessBarreiro,Eliezer J.Fraga,Carlos A. M.Miranda,Ana L. P.Rodrigues,Carlos R.por2002-07-31T00:00:00Zoai:scielo:S0100-40422002000100022Revistahttps://www.scielo.br/j/qn/ONGhttps://old.scielo.br/oai/scielo-oai.phpquimicanova@sbq.org.br1678-70640100-4042opendoar:2002-07-31T00:00Química Nova (Online) - Sociedade Brasileira de Química (SBQ)false
dc.title.none.fl_str_mv A química medicinal de N-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticos
title A química medicinal de N-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticos
spellingShingle A química medicinal de N-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticos
Barreiro,Eliezer J.
bioactive N-acylhydrazones derivatives
antiinflammatory, analgesic and antithrombotic properties
molecular hybridization and bioisosterism in drug design
title_short A química medicinal de N-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticos
title_full A química medicinal de N-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticos
title_fullStr A química medicinal de N-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticos
title_full_unstemmed A química medicinal de N-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticos
title_sort A química medicinal de N-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticos
author Barreiro,Eliezer J.
author_facet Barreiro,Eliezer J.
Fraga,Carlos A. M.
Miranda,Ana L. P.
Rodrigues,Carlos R.
author_role author
author2 Fraga,Carlos A. M.
Miranda,Ana L. P.
Rodrigues,Carlos R.
author2_role author
author
author
dc.contributor.author.fl_str_mv Barreiro,Eliezer J.
Fraga,Carlos A. M.
Miranda,Ana L. P.
Rodrigues,Carlos R.
dc.subject.por.fl_str_mv bioactive N-acylhydrazones derivatives
antiinflammatory, analgesic and antithrombotic properties
molecular hybridization and bioisosterism in drug design
topic bioactive N-acylhydrazones derivatives
antiinflammatory, analgesic and antithrombotic properties
molecular hybridization and bioisosterism in drug design
description In this article are described new bioactive N-acylhydrazone (NAH) derivatives, structurally designed as optimization of aryl hydrazones precursors planned by molecular hybridization of two 5-lipoxigenase inhibitors, e.g. CBS-1108 and BW-755c. The analgesic, antiedematogenic and anti-platelet aggregating profile of several isosteric compounds was investigated by using classic pharmacological assays in vivo and ex-vivo, allowing to identify new potent peripheric analgesic lead, a new anti-inflammatory and an antithrombotic agent. During this study was discovered dozen of active NAH compounds clarifying the structure-activity relationship for this series of NAH derivatives, indicating the pharmacophore character of the N-acylhydrazone functionality.
publishDate 2002
dc.date.none.fl_str_mv 2002-02-01
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-40422002000100022
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0100-40422002000100022
dc.language.iso.fl_str_mv por
language por
dc.relation.none.fl_str_mv 10.1590/S0100-40422002000100022
dc.rights.driver.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv text/html
dc.publisher.none.fl_str_mv Sociedade Brasileira de Química
publisher.none.fl_str_mv Sociedade Brasileira de Química
dc.source.none.fl_str_mv Química Nova v.25 n.1 2002
reponame:Química Nova (Online)
instname:Sociedade Brasileira de Química (SBQ)
instacron:SBQ
instname_str Sociedade Brasileira de Química (SBQ)
instacron_str SBQ
institution SBQ
reponame_str Química Nova (Online)
collection Química Nova (Online)
repository.name.fl_str_mv Química Nova (Online) - Sociedade Brasileira de Química (SBQ)
repository.mail.fl_str_mv quimicanova@sbq.org.br
_version_ 1750318102383427584