STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF DITERPENES FOR TREATMENT OF ALZHEIMER'S DISEASE
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...
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| Format: | Article |
| Language: | English |
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Sociedade Brasileira de Química
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| Series: | Química Nova |
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| Online Access: | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-40422017000901045&lng=en&tlng=en |
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| author | Gabriel F. dos Santos Rondinelle G. Pereira Maria A. D. Boaventura Francisco A. Macias Gesiane da S. Lima Amanda C. S. Coelho Jose M. G. Molinillo Antonio Cala Jacqueline A. Takahashi |
| author_facet | Gabriel F. dos Santos Rondinelle G. Pereira Maria A. D. Boaventura Francisco A. Macias Gesiane da S. Lima Amanda C. S. Coelho Jose M. G. Molinillo Antonio Cala Jacqueline A. Takahashi |
| author_sort | Gabriel F. dos Santos |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-12-10T08:41:13Z |
| format | Article |
| id | doaj.art-15a9a2a9b7354f0fbae7195a14e2e4ab |
| institution | Directory Open Access Journal |
| issn | 1678-7064 |
| language | English |
| last_indexed | 2024-12-10T08:41:13Z |
| publisher | Sociedade Brasileira de Química |
| record_format | Article |
| series | Química Nova |
| spelling | doaj.art-15a9a2a9b7354f0fbae7195a14e2e4ab2022-12-22T01:55:50ZengSociedade Brasileira de QuímicaQuímica Nova1678-70644091045105010.21577/0100-4042.20170112S0100-40422017000901045STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF DITERPENES FOR TREATMENT OF ALZHEIMER'S DISEASEGabriel F. dos SantosRondinelle G. PereiraMaria A. D. BoaventuraFrancisco A. MaciasGesiane da S. LimaAmanda C. S. CoelhoJose M. G. MolinilloAntonio CalaJacqueline A. TakahashiAlzheimer'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.http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-40422017000901045&lng=en&tlng=enkaurane diterpenesacetylcholinesterase inhibitorsAlzheimer's disease |
| spellingShingle | Gabriel F. dos Santos Rondinelle G. Pereira Maria A. D. Boaventura Francisco A. Macias Gesiane da S. Lima Amanda C. S. Coelho Jose M. G. Molinillo Antonio Cala Jacqueline A. Takahashi STRUCTURE-ACTIVITY RELATIONSHIP STUDY OF DITERPENES FOR TREATMENT OF ALZHEIMER'S DISEASE Química Nova kaurane diterpenes acetylcholinesterase inhibitors Alzheimer's disease |
| title | 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_short | 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 |
| topic | kaurane diterpenes acetylcholinesterase inhibitors Alzheimer's disease |
| url | http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-40422017000901045&lng=en&tlng=en |
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