Structure-activity relationship study of diterpenes for treatment of Alzheimer's disease

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dc.creatorGabriel Franco dos Santos
dc.creatorRondinelle Gomes Pereira
dc.creatorMaria Amélia Diamantino Boaventura
dc.creatorFrancisco a Macias
dc.creatorGesiane da Silva Lima
dc.creatorAmanda Cristina Soares Coelho
dc.creatorJosé María González Molinillo
dc.creatorAntonio Cala
dc.creatorJacqueline Aparecida Takahashi
dc.date.accessioned2023-10-09T23:18:49Z
dc.date.accessioned2025-09-09T01:17:19Z
dc.date.available2023-10-09T23:18:49Z
dc.date.issued2017
dc.description.sponsorshipCNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológico
dc.description.sponsorshipFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas Gerais
dc.description.sponsorshipCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
dc.format.mimetypepdf
dc.identifier.doihttps://doi.org/10.21577/0100-4042.20170112
dc.identifier.issn0100-4042
dc.identifier.urihttps://hdl.handle.net/1843/59342
dc.languageeng
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofQuímica Nova
dc.rightsAcesso Aberto
dc.subjectDiterpenos
dc.subjectAlzheimer, Doença de
dc.subject.otherKaurane diterpenes
dc.subject.otherAcetylcholinesterase inhibitors
dc.subject.otherAlzheimer's disease
dc.titleStructure-activity relationship study of diterpenes for treatment of Alzheimer's disease
dc.typeArtigo de periódico
local.citation.epage1050
local.citation.issue9
local.citation.spage1045
local.citation.volume40
local.description.resumoAlzheimer's disease is an irreversible, degenerative and age-related disease which is growing more and more with the increase in life expectancy. Kaurane diterpenes are a class of natural products available in large amounts in nature and isolated from plants grown worldwide. In the present work¸ twenty-seven kaurane diterpenes of natural origin and some readily available derivatives were assayed for acetylcholinesterase inhibition and the structure-activity relationship was analyzed. The kaurenoic acid derivatives screened showed to be promising inhibitors of AChE, which could provide new leads for drugs to fight Alzheimer's disease symptoms. Among them, eleven compounds showed activities comparable or higher than the positive control galantamine. Existence of an allylic hydroxyl group showed to be an important structural feature for AChE inhibition. In addition, presence of free hydroxyl groups at C-17 and C-19, furnished a diol especially active, able to completely inhibit AChE.
local.identifier.orcidhttps://orcid.org/0000-0003-4651-3840
local.publisher.countryBrasil
local.publisher.departmentICX - DEPARTAMENTO DE QUÍMICA
local.publisher.initialsUFMG
local.url.externahttps://www.scielo.br/j/qn/a/GDtjZBmh8pWMyzyRBSQLd6S/

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