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http://hdl.handle.net/1843/59342| Type: | Artigo de Periódico |
| Title: | Structure-activity relationship study of diterpenes for treatment of Alzheimer's disease |
| Authors: | 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 |
| Abstract: | Alzheimer'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. |
| Subject: | Diterpenos Alzheimer, Doença de |
| language: | eng |
| metadata.dc.publisher.country: | Brasil |
| Publisher: | Universidade Federal de Minas Gerais |
| Publisher Initials: | UFMG |
| metadata.dc.publisher.department: | ICX - DEPARTAMENTO DE QUÍMICA |
| Rights: | Acesso Aberto |
| metadata.dc.identifier.doi: | https://doi.org/10.21577/0100-4042.20170112 |
| URI: | http://hdl.handle.net/1843/59342 |
| Issue Date: | 2017 |
| metadata.dc.url.externa: | https://www.scielo.br/j/qn/a/GDtjZBmh8pWMyzyRBSQLd6S/ |
| metadata.dc.relation.ispartof: | Química Nova |
| Appears in Collections: | Artigo de Periódico |
Files in This Item:
| File | Description | Size | Format | |
|---|---|---|---|---|
| STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF DITERPENES FOR TREATMENT OF ALZHEIMER'S DISEASE.pdf | 268.49 kB | Adobe PDF | View/Open |
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