New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity

Detalhes bibliográficos
Autor(a) principal: SALVADOR,RAQUEL R.S.
Data de Publicação: 2016
Outros Autores: BELLO,MURILO L., BARRETO,IGOR R.L., VERA,MARIA A.F., MURI,ESTELA M.F., ALBUQUERQUE,SÉRGIO DE, DIAS,LUIZA R.S.
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Anais da Academia Brasileira de Ciências (Online)
Texto Completo: http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652016000602341
Resumo: ABSTRACT This paper reports the in vitro trypanocidal activity evaluation of new carbohydrazide derivatives from 3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridine, substituted at C-6 position by phenyl, methyl or trifluoromethyl group. These compounds were evaluated in order to identify the antiparasitic profile against trypomastigote and amastigote forms of Trypanosoma cruzi. The 4-carbohydrazide derivatives presented different profiles of activity. In the investigation of the chemical structure influence in the trypanocidal activity, the results indicated there are large lipophilicity and volume differences among these derivatives. The complementarities of their stereoelectronic and physical-chemical aspects seem to be relevant for the biological activity against T. cruzi.
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spelling New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity1H-pyrazolo[3,4-b]pyridinecarbohydrazide derivativesbiological activitiestrypanocidal activitymolecular modelingABSTRACT This paper reports the in vitro trypanocidal activity evaluation of new carbohydrazide derivatives from 3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridine, substituted at C-6 position by phenyl, methyl or trifluoromethyl group. These compounds were evaluated in order to identify the antiparasitic profile against trypomastigote and amastigote forms of Trypanosoma cruzi. The 4-carbohydrazide derivatives presented different profiles of activity. In the investigation of the chemical structure influence in the trypanocidal activity, the results indicated there are large lipophilicity and volume differences among these derivatives. The complementarities of their stereoelectronic and physical-chemical aspects seem to be relevant for the biological activity against T. cruzi.Academia Brasileira de Ciências2016-12-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652016000602341Anais da Academia Brasileira de Ciências v.88 n.4 2016reponame:Anais da Academia Brasileira de Ciências (Online)instname:Academia Brasileira de Ciências (ABC)instacron:ABC10.1590/0001-3765201620160087info:eu-repo/semantics/openAccessSALVADOR,RAQUEL R.S.BELLO,MURILO L.BARRETO,IGOR R.L.VERA,MARIA A.F.MURI,ESTELA M.F.ALBUQUERQUE,SÉRGIO DEDIAS,LUIZA R.S.eng2017-06-12T00:00:00Zoai:scielo:S0001-37652016000602341Revistahttp://www.scielo.br/aabchttps://old.scielo.br/oai/scielo-oai.php||aabc@abc.org.br1678-26900001-3765opendoar:2017-06-12T00:00Anais da Academia Brasileira de Ciências (Online) - Academia Brasileira de Ciências (ABC)false
dc.title.none.fl_str_mv New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity
title New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity
spellingShingle New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity
SALVADOR,RAQUEL R.S.
1H-pyrazolo[3,4-b]pyridine
carbohydrazide derivatives
biological activities
trypanocidal activity
molecular modeling
title_short New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity
title_full New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity
title_fullStr New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity
title_full_unstemmed New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity
title_sort New carbohydrazide derivatives of 1H-pyrazolo[3,4-b]pyridine and trypanocidal activity
author SALVADOR,RAQUEL R.S.
author_facet SALVADOR,RAQUEL R.S.
BELLO,MURILO L.
BARRETO,IGOR R.L.
VERA,MARIA A.F.
MURI,ESTELA M.F.
ALBUQUERQUE,SÉRGIO DE
DIAS,LUIZA R.S.
author_role author
author2 BELLO,MURILO L.
BARRETO,IGOR R.L.
VERA,MARIA A.F.
MURI,ESTELA M.F.
ALBUQUERQUE,SÉRGIO DE
DIAS,LUIZA R.S.
author2_role author
author
author
author
author
author
dc.contributor.author.fl_str_mv SALVADOR,RAQUEL R.S.
BELLO,MURILO L.
BARRETO,IGOR R.L.
VERA,MARIA A.F.
MURI,ESTELA M.F.
ALBUQUERQUE,SÉRGIO DE
DIAS,LUIZA R.S.
dc.subject.por.fl_str_mv 1H-pyrazolo[3,4-b]pyridine
carbohydrazide derivatives
biological activities
trypanocidal activity
molecular modeling
topic 1H-pyrazolo[3,4-b]pyridine
carbohydrazide derivatives
biological activities
trypanocidal activity
molecular modeling
description ABSTRACT This paper reports the in vitro trypanocidal activity evaluation of new carbohydrazide derivatives from 3-methyl-1-phenyl-1H-pyrazolo[3,4-b]pyridine, substituted at C-6 position by phenyl, methyl or trifluoromethyl group. These compounds were evaluated in order to identify the antiparasitic profile against trypomastigote and amastigote forms of Trypanosoma cruzi. The 4-carbohydrazide derivatives presented different profiles of activity. In the investigation of the chemical structure influence in the trypanocidal activity, the results indicated there are large lipophilicity and volume differences among these derivatives. The complementarities of their stereoelectronic and physical-chemical aspects seem to be relevant for the biological activity against T. cruzi.
publishDate 2016
dc.date.none.fl_str_mv 2016-12-01
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=S0001-37652016000602341
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0001-37652016000602341
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 10.1590/0001-3765201620160087
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 Academia Brasileira de Ciências
publisher.none.fl_str_mv Academia Brasileira de Ciências
dc.source.none.fl_str_mv Anais da Academia Brasileira de Ciências v.88 n.4 2016
reponame:Anais da Academia Brasileira de Ciências (Online)
instname:Academia Brasileira de Ciências (ABC)
instacron:ABC
instname_str Academia Brasileira de Ciências (ABC)
instacron_str ABC
institution ABC
reponame_str Anais da Academia Brasileira de Ciências (Online)
collection Anais da Academia Brasileira de Ciências (Online)
repository.name.fl_str_mv Anais da Academia Brasileira de Ciências (Online) - Academia Brasileira de Ciências (ABC)
repository.mail.fl_str_mv ||aabc@abc.org.br
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