New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids

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dc.contributor.authorViegas, C.
dc.contributor.authorBolzani, Vanderlan da Silva [UNESP]
dc.contributor.authorPimentel, LSB
dc.contributor.authorCastro, N. G.
dc.contributor.authorCabral, R. F.
dc.contributor.authorCosta, R. S.
dc.contributor.authorFloyd, C.
dc.contributor.authorRocha, M. S.
dc.contributor.authorYoung, MCM
dc.contributor.authorBarreiro, E. J.
dc.contributor.authorFraga, CAM
dc.contributor.institutionUniversidade Federal do Rio de Janeiro (UFRJ)
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionInst Bot
dc.date.accessioned2014-05-20T15:22:50Z
dc.date.available2014-05-20T15:22:50Z
dc.date.issued2005-07-01
dc.description.abstractFive new piperidine alkaloids were designed from natural (-)-3-O-acetyl-spectaline and (-)-spectaline that were obtained from the flowers of Senna spectabilis (sin. Cassia spectabilis, Leguminosae). Two semi-synthetic analogues (7 and 9) inhibited rat brain acetylcholinesterase, showing IC50 of 7.32 and 15.1 mu M, and were 21 and 9.5 times less potent against rat brain butyrylcholinesterase, respectively. Compound 9 (1 mg/kg, ip) was fully efficacious in reverting scopolamine-induced amnesia in mice. The two active compounds (7 and 9) did not show overt toxic effects at the doses tested in vivo. (c) 2005 Elsevier Ltd. All rights reserved.en
dc.description.affiliationUniv Fed Rio de Janeiro, Fac Farm, Lab Avaliacao & Sintese Substancias Bioativas, BR-21944910 Rio de Janeiro, Brazil
dc.description.affiliationUniv Estadual Paulista, Inst Quim, NuBBE, BR-14801970 Araraquara, Brazil
dc.description.affiliationUniv Fed Rio de Janeiro, Inst Ciências Biomed, Ctr Ciências Saude, Dept FArmacol Basica & Clin, Rio de Janeiro, Brazil
dc.description.affiliationInst Bot, Secao Bioquim & Fisiol Plantas, São Paulo, Brazil
dc.description.affiliationUnespUniv Estadual Paulista, Inst Quim, NuBBE, BR-14801970 Araraquara, Brazil
dc.format.extent4184-4190
dc.identifierhttp://dx.doi.org/10.1016/j.bmc.2005.04.030
dc.identifier.citationBioorganic & Medicinal Chemistry. Oxford: Pergamon-Elsevier B.V., v. 13, n. 13, p. 4184-4190, 2005.
dc.identifier.doi10.1016/j.bmc.2005.04.030
dc.identifier.issn0968-0896
dc.identifier.lattes4484083685251673
dc.identifier.urihttp://hdl.handle.net/11449/33748
dc.identifier.wosWOS:000229811900006
dc.language.isoeng
dc.publisherElsevier B.V.
dc.relation.ispartofBioorganic & Medicinal Chemistry
dc.relation.ispartofjcr2.881
dc.relation.ispartofsjr0,871
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.subjectpiperidine alkaloidspt
dc.subjectacetylcholinesterase inhibitorspt
dc.subjectAlzheimer's diseasept
dc.subjectSenna spectabilispt
dc.titleNew selective acetylcholinesterase inhibitors designed from natural piperidine alkaloidsen
dc.typeArtigo
dcterms.licensehttp://www.elsevier.com/about/open-access/open-access-policies/article-posting-policy
dcterms.rightsHolderElsevier B.V.
unesp.author.lattes4484083685251673
unesp.campusUniversidade Estadual Paulista (Unesp), Instituto de Química, Araraquarapt
unesp.departmentQuímica Orgânica - IQARpt

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