Xanthone and Flavone Derivatives as Dual Agents with Acetylcholinesterase Inhibition and Antioxidant Activity as Potential Anti-Alzheimer Agents
Alzheimer’s disease (AD) is a multifactorial neurodegenerative disorder that is associated with the elderly. The current therapy that is used to treat AD is based mainly on the administration of acetylcholinesterase (AChE) inhibitors. Due to their low efficacy there is a considerable need for other...
Saved in:
| Main Authors: | , , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
Wiley
2017-01-01
|
| Series: | Journal of Chemistry |
| Online Access: | http://dx.doi.org/10.1155/2017/8587260 |
| Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
| _version_ | 1832556772232003584 |
|---|---|
| author | Inês Cruz Ploenthip Puthongking Sara Cravo Andreia Palmeira Honorina Cidade Madalena Pinto Emília Sousa |
| author_facet | Inês Cruz Ploenthip Puthongking Sara Cravo Andreia Palmeira Honorina Cidade Madalena Pinto Emília Sousa |
| author_sort | Inês Cruz |
| collection | DOAJ |
| description | Alzheimer’s disease (AD) is a multifactorial neurodegenerative disorder that is associated with the elderly. The current therapy that is used to treat AD is based mainly on the administration of acetylcholinesterase (AChE) inhibitors. Due to their low efficacy there is a considerable need for other therapeutic strategies. Considering that the malfunctions of different, but interconnected, biochemical complex pathways play an important role in the pathogenesis of this disease, a promising therapy may consist in administration of drugs that act on more than a target on biochemical scenery of AD. In this work, the synthesis and evaluation of xanthone and flavone derivatives as antioxidants with AChE inhibitory activity were accomplished. Among the obtained compounds, Mannich bases 3 and 14 showed capacity to inhibit AChE and antioxidant property, exerting dual activity. Moreover, for the most promising AChE inhibitors, docking studies on the target have been performed aiming to predict the binding mechanism. The results presented here may help to identify new xanthone and flavone derivatives as dual anti-Alzheimer agents with AChE inhibitory and antioxidant activities. |
| format | Article |
| id | doaj-art-bad213588a7f4fe2bd0185e155d47cd4 |
| institution | Kabale University |
| issn | 2090-9063 2090-9071 |
| language | English |
| publishDate | 2017-01-01 |
| publisher | Wiley |
| record_format | Article |
| series | Journal of Chemistry |
| spelling | doaj-art-bad213588a7f4fe2bd0185e155d47cd42025-02-03T05:44:26ZengWileyJournal of Chemistry2090-90632090-90712017-01-01201710.1155/2017/85872608587260Xanthone and Flavone Derivatives as Dual Agents with Acetylcholinesterase Inhibition and Antioxidant Activity as Potential Anti-Alzheimer AgentsInês Cruz0Ploenthip Puthongking1Sara Cravo2Andreia Palmeira3Honorina Cidade4Madalena Pinto5Emília Sousa6Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, PortugalFaculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, ThailandLaboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, PortugalLaboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, PortugalLaboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, PortugalLaboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, PortugalLaboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua de Jorge Viterbo Ferreira 228, 4050-313 Porto, PortugalAlzheimer’s disease (AD) is a multifactorial neurodegenerative disorder that is associated with the elderly. The current therapy that is used to treat AD is based mainly on the administration of acetylcholinesterase (AChE) inhibitors. Due to their low efficacy there is a considerable need for other therapeutic strategies. Considering that the malfunctions of different, but interconnected, biochemical complex pathways play an important role in the pathogenesis of this disease, a promising therapy may consist in administration of drugs that act on more than a target on biochemical scenery of AD. In this work, the synthesis and evaluation of xanthone and flavone derivatives as antioxidants with AChE inhibitory activity were accomplished. Among the obtained compounds, Mannich bases 3 and 14 showed capacity to inhibit AChE and antioxidant property, exerting dual activity. Moreover, for the most promising AChE inhibitors, docking studies on the target have been performed aiming to predict the binding mechanism. The results presented here may help to identify new xanthone and flavone derivatives as dual anti-Alzheimer agents with AChE inhibitory and antioxidant activities.http://dx.doi.org/10.1155/2017/8587260 |
| spellingShingle | Inês Cruz Ploenthip Puthongking Sara Cravo Andreia Palmeira Honorina Cidade Madalena Pinto Emília Sousa Xanthone and Flavone Derivatives as Dual Agents with Acetylcholinesterase Inhibition and Antioxidant Activity as Potential Anti-Alzheimer Agents Journal of Chemistry |
| title | Xanthone and Flavone Derivatives as Dual Agents with Acetylcholinesterase Inhibition and Antioxidant Activity as Potential Anti-Alzheimer Agents |
| title_full | Xanthone and Flavone Derivatives as Dual Agents with Acetylcholinesterase Inhibition and Antioxidant Activity as Potential Anti-Alzheimer Agents |
| title_fullStr | Xanthone and Flavone Derivatives as Dual Agents with Acetylcholinesterase Inhibition and Antioxidant Activity as Potential Anti-Alzheimer Agents |
| title_full_unstemmed | Xanthone and Flavone Derivatives as Dual Agents with Acetylcholinesterase Inhibition and Antioxidant Activity as Potential Anti-Alzheimer Agents |
| title_short | Xanthone and Flavone Derivatives as Dual Agents with Acetylcholinesterase Inhibition and Antioxidant Activity as Potential Anti-Alzheimer Agents |
| title_sort | xanthone and flavone derivatives as dual agents with acetylcholinesterase inhibition and antioxidant activity as potential anti alzheimer agents |
| url | http://dx.doi.org/10.1155/2017/8587260 |
| work_keys_str_mv | AT inescruz xanthoneandflavonederivativesasdualagentswithacetylcholinesteraseinhibitionandantioxidantactivityaspotentialantialzheimeragents AT ploenthipputhongking xanthoneandflavonederivativesasdualagentswithacetylcholinesteraseinhibitionandantioxidantactivityaspotentialantialzheimeragents AT saracravo xanthoneandflavonederivativesasdualagentswithacetylcholinesteraseinhibitionandantioxidantactivityaspotentialantialzheimeragents AT andreiapalmeira xanthoneandflavonederivativesasdualagentswithacetylcholinesteraseinhibitionandantioxidantactivityaspotentialantialzheimeragents AT honorinacidade xanthoneandflavonederivativesasdualagentswithacetylcholinesteraseinhibitionandantioxidantactivityaspotentialantialzheimeragents AT madalenapinto xanthoneandflavonederivativesasdualagentswithacetylcholinesteraseinhibitionandantioxidantactivityaspotentialantialzheimeragents AT emiliasousa xanthoneandflavonederivativesasdualagentswithacetylcholinesteraseinhibitionandantioxidantactivityaspotentialantialzheimeragents |