Design, synthesis and anticonvulsant activity evaluation of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives

Detalhes bibliográficos
Autor(a) principal: Sun,Xian-Yu
Data de Publicação: 2009
Outros Autores: Guan,Li-Ping, Zhang,Lei, Wei,Cheng-Xi, Piao,Hu-Ri, Quan,Zhe-Shan
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=S0103-50532009000500004
Resumo: In this study, a novel series of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives was synthesized as potential anticonvulsant agents. Their anticonvulsant activities were evaluated by the maximal electroshock (MES) test, and their neurotoxicities were evaluated by the rotarod neurotoxicity test. The pharmacological results showed that 7-hexyloxy-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one 4e was the most potent with median effective dose (ED50) value of 6.6 mg kg-1, median toxicity dose (TD50) of 39.4 mg kg-1, providing a protective index (PI=TD50 /ED50) value of 6.0.
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spelling Design, synthesis and anticonvulsant activity evaluation of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivativestriazinophthalazineanticonvulsantneurotoxicityIn this study, a novel series of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives was synthesized as potential anticonvulsant agents. Their anticonvulsant activities were evaluated by the maximal electroshock (MES) test, and their neurotoxicities were evaluated by the rotarod neurotoxicity test. The pharmacological results showed that 7-hexyloxy-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one 4e was the most potent with median effective dose (ED50) value of 6.6 mg kg-1, median toxicity dose (TD50) of 39.4 mg kg-1, providing a protective index (PI=TD50 /ED50) value of 6.0.Sociedade Brasileira de Química2009-01-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersiontext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532009000500004Journal of the Brazilian Chemical Society v.20 n.5 2009reponame:Journal of the Brazilian Chemical Society (Online)instname:Sociedade Brasileira de Química (SBQ)instacron:SBQ10.1590/S0103-50532009000500004info:eu-repo/semantics/openAccessSun,Xian-YuGuan,Li-PingZhang,LeiWei,Cheng-XiPiao,Hu-RiQuan,Zhe-Shaneng2009-06-29T00:00:00Zoai:scielo:S0103-50532009000500004Revistahttp://jbcs.sbq.org.brONGhttps://old.scielo.br/oai/scielo-oai.php||office@jbcs.sbq.org.br1678-47900103-5053opendoar:2009-06-29T00:00Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ)false
dc.title.none.fl_str_mv Design, synthesis and anticonvulsant activity evaluation of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives
title Design, synthesis and anticonvulsant activity evaluation of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives
spellingShingle Design, synthesis and anticonvulsant activity evaluation of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives
Sun,Xian-Yu
triazino
phthalazine
anticonvulsant
neurotoxicity
title_short Design, synthesis and anticonvulsant activity evaluation of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives
title_full Design, synthesis and anticonvulsant activity evaluation of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives
title_fullStr Design, synthesis and anticonvulsant activity evaluation of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives
title_full_unstemmed Design, synthesis and anticonvulsant activity evaluation of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives
title_sort Design, synthesis and anticonvulsant activity evaluation of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives
author Sun,Xian-Yu
author_facet Sun,Xian-Yu
Guan,Li-Ping
Zhang,Lei
Wei,Cheng-Xi
Piao,Hu-Ri
Quan,Zhe-Shan
author_role author
author2 Guan,Li-Ping
Zhang,Lei
Wei,Cheng-Xi
Piao,Hu-Ri
Quan,Zhe-Shan
author2_role author
author
author
author
author
dc.contributor.author.fl_str_mv Sun,Xian-Yu
Guan,Li-Ping
Zhang,Lei
Wei,Cheng-Xi
Piao,Hu-Ri
Quan,Zhe-Shan
dc.subject.por.fl_str_mv triazino
phthalazine
anticonvulsant
neurotoxicity
topic triazino
phthalazine
anticonvulsant
neurotoxicity
description In this study, a novel series of 7-substituted-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one derivatives was synthesized as potential anticonvulsant agents. Their anticonvulsant activities were evaluated by the maximal electroshock (MES) test, and their neurotoxicities were evaluated by the rotarod neurotoxicity test. The pharmacological results showed that 7-hexyloxy-4H-[1,2,4]triazino[3,4-a]phthalazin-4-one 4e was the most potent with median effective dose (ED50) value of 6.6 mg kg-1, median toxicity dose (TD50) of 39.4 mg kg-1, providing a protective index (PI=TD50 /ED50) value of 6.0.
publishDate 2009
dc.date.none.fl_str_mv 2009-01-01
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
format article
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dc.identifier.uri.fl_str_mv http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532009000500004
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532009000500004
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv 10.1590/S0103-50532009000500004
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 Journal of the Brazilian Chemical Society v.20 n.5 2009
reponame:Journal of the Brazilian Chemical Society (Online)
instname:Sociedade Brasileira de Química (SBQ)
instacron:SBQ
instname_str Sociedade Brasileira de Química (SBQ)
instacron_str SBQ
institution SBQ
reponame_str Journal of the Brazilian Chemical Society (Online)
collection Journal of the Brazilian Chemical Society (Online)
repository.name.fl_str_mv Journal of the Brazilian Chemical Society (Online) - Sociedade Brasileira de Química (SBQ)
repository.mail.fl_str_mv ||office@jbcs.sbq.org.br
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