Structure-activity relationship study of diterpenes for treatment of Alzheimer's disease
| Autor(a) principal: | |
|---|---|
| Data de Publicação: | 2017 |
| Outros Autores: | , , , , , , , |
| Tipo de documento: | Artigo |
| Idioma: | eng |
| Título da fonte: | Repositório Institucional da UFMG |
| Texto Completo: | https://doi.org/10.21577/0100-4042.20170112 http://hdl.handle.net/1843/59342 https://orcid.org/0000-0003-4651-3840 |
Resumo: | CNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológico |
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2023-10-09T23:18:49Z2023-10-09T23:18:49Z201740910451050https://doi.org/10.21577/0100-4042.201701120100-4042http://hdl.handle.net/1843/59342https://orcid.org/0000-0003-4651-3840CNPq - Conselho Nacional de Desenvolvimento Científico e TecnológicoFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas GeraisCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível SuperiorAlzheimer'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.engUniversidade Federal de Minas GeraisUFMGBrasilICX - DEPARTAMENTO DE QUÍMICAQuímica NovaDiterpenosAlzheimer, Doença deKaurane diterpenesAcetylcholinesterase inhibitorsAlzheimer's diseaseStructure-activity relationship study of diterpenes for treatment of Alzheimer's diseaseinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttps://www.scielo.br/j/qn/a/GDtjZBmh8pWMyzyRBSQLd6S/Gabriel Franco dos SantosRondinelle Gomes PereiraMaria Amélia Diamantino BoaventuraFrancisco a MaciasGesiane da Silva LimaAmanda Cristina Soares CoelhoJosé María González MolinilloAntonio CalaJacqueline Aparecida Takahashiapplication/pdfinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da UFMGinstname:Universidade Federal de Minas Gerais (UFMG)instacron:UFMGLICENSELicense.txtLicense.txttext/plain; charset=utf-82042https://repositorio.ufmg.br/bitstream/1843/59342/1/License.txtfa505098d172de0bc8864fc1287ffe22MD51ORIGINALSTRUCTURE-ACTIVITY RELATIONSHIP STUDY OF DITERPENES FOR TREATMENT OF ALZHEIMER'S DISEASE.pdfSTRUCTURE-ACTIVITY RELATIONSHIP STUDY OF DITERPENES FOR TREATMENT OF ALZHEIMER'S DISEASE.pdfapplication/pdf274935https://repositorio.ufmg.br/bitstream/1843/59342/2/STRUCTURE-ACTIVITY%20RELATIONSHIP%20STUDY%20OF%20DITERPENES%20FOR%20TREATMENT%20OF%20ALZHEIMER%27S%20DISEASE.pdfd94c8844a4b626a65f7260fb66b8d901MD521843/593422023-10-09 20:18:49.459oai:repositorio.ufmg.br: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Repositório de PublicaçõesPUBhttps://repositorio.ufmg.br/oaiopendoar:2023-10-09T23:18:49Repositório Institucional da UFMG - Universidade Federal de Minas Gerais (UFMG)false |
| dc.title.pt_BR.fl_str_mv |
Structure-activity relationship study of diterpenes for treatment of Alzheimer's disease |
| title |
Structure-activity relationship study of diterpenes for treatment of Alzheimer's disease |
| spellingShingle |
Structure-activity relationship study of diterpenes for treatment of Alzheimer's disease Gabriel Franco dos Santos Kaurane diterpenes Acetylcholinesterase inhibitors Alzheimer's disease Diterpenos Alzheimer, Doença de |
| title_short |
Structure-activity relationship study of diterpenes for treatment of Alzheimer's disease |
| title_full |
Structure-activity relationship study of diterpenes for treatment of Alzheimer's disease |
| title_fullStr |
Structure-activity relationship study of diterpenes for treatment of Alzheimer's disease |
| title_full_unstemmed |
Structure-activity relationship study of diterpenes for treatment of Alzheimer's disease |
| title_sort |
Structure-activity relationship study of diterpenes for treatment of Alzheimer's disease |
| author |
Gabriel Franco dos Santos |
| author_facet |
Gabriel Franco dos Santos Rondinelle Gomes Pereira Maria Amélia Diamantino Boaventura Francisco a Macias Gesiane da Silva Lima Amanda Cristina Soares Coelho José María González Molinillo Antonio Cala Jacqueline Aparecida Takahashi |
| author_role |
author |
| author2 |
Rondinelle Gomes Pereira Maria Amélia Diamantino Boaventura Francisco a Macias Gesiane da Silva Lima Amanda Cristina Soares Coelho José María González Molinillo Antonio Cala Jacqueline Aparecida Takahashi |
| author2_role |
author author author author author author author author |
| dc.contributor.author.fl_str_mv |
Gabriel Franco dos Santos Rondinelle Gomes Pereira Maria Amélia Diamantino Boaventura Francisco a Macias Gesiane da Silva Lima Amanda Cristina Soares Coelho José María González Molinillo Antonio Cala Jacqueline Aparecida Takahashi |
| dc.subject.por.fl_str_mv |
Kaurane diterpenes Acetylcholinesterase inhibitors Alzheimer's disease |
| topic |
Kaurane diterpenes Acetylcholinesterase inhibitors Alzheimer's disease Diterpenos Alzheimer, Doença de |
| dc.subject.other.pt_BR.fl_str_mv |
Diterpenos Alzheimer, Doença de |
| description |
CNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológico |
| publishDate |
2017 |
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2017 |
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2023-10-09T23:18:49Z |
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2023-10-09T23:18:49Z |
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info:eu-repo/semantics/publishedVersion |
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info:eu-repo/semantics/article |
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article |
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http://hdl.handle.net/1843/59342 |
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https://doi.org/10.21577/0100-4042.20170112 |
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0100-4042 |
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https://orcid.org/0000-0003-4651-3840 |
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eng |
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Química Nova |
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Universidade Federal de Minas Gerais |
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UFMG |
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Brasil |
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ICX - DEPARTAMENTO DE QUÍMICA |
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Universidade Federal de Minas Gerais |
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