New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids

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dc.TypeArticlept_BR
dc.contributor.authorViegas Junior, Claudio
dc.contributor.authorBolzani, Vanderlan da Silva
dc.contributor.authorPimentel, Luísa Sá Barreto
dc.contributor.authorCastro, Newton Gonçalves de
dc.contributor.authorCabral, Rafael Ferreira Pacheco
dc.contributor.authorFloyd, Corinne
dc.contributor.authorYoung, Maria Cláudia Marx
dc.contributor.authorBarreiro, Eliezer Jesus de Lacerda
dc.contributor.authorFraga, Carlos Alberto Manssour
dc.contributor.authorRocha, Monica Santos
dc.contributor.authorCosta, Rodrigo Saar da
dc.date.accessioned2022-03-11T17:00:53Z
dc.date.available2022-03-11T17:00:53Z
dc.date.issued2005
dc.descriptionp. 4184-4190.: il. p&b.
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 microM, and were 21 and 9.5 times less potent against rat brain butyrylcholinesterase, respectively. Compound 9 (1mg/kg, i.p.) 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.
dc.identifier.citationVIEGAS JUNIOR, Claudio et al. New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids. Bioorganic & Medicinal Chemistry, v. 13, p. 4184-4190, 2005.
dc.identifier.issn1464-3391
dc.identifier.urihttp://sr-vmlxaph03:8080/jspui/handle/123456789/5629
dc.publisherBioorganic & Medicinal Chemistrypt_BR
dc.subjectInhibidores de la Colinesterasapt_BR
dc.subjectAlcaloidespt_BR
dc.subjectAlkaloidspt_BR
dc.subjectInibidores da Colinesterasept_BR
dc.subjectCholinesterase Inhibitorspt_BR
dc.subjectPiperidínicos naturais
dc.titleNew selective acetylcholinesterase inhibitors designed from natural piperidine alkaloidspt_BR

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