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Synthesis and Study of a Selected Series of Amides with the Coumarin Scaffold for the Treatment of Alzheimer's Disease
* 1, 2 , 1, 2 , 3, 4 , 1 , 2 , 2 , 4 , 4
1  CIQUP/Departamento de Química e Bioquímica, Faculdade de Ciências, Universidade do Porto, 4169-007 Porto, Portugal
2  Departamento de Química Orgánica, Facultad de Farmacia, Universidad de Santiago de Compostela, 15782 Santiago de Compostela, Spain
3  Facultad de Farmacia de Universidad de Santiago de Compostela
4  Instituto de Química de Recursos Naturales, Universidad de Talca

Abstract: Due to the synthetic accessibility of different substituted coumarins and their biological properties, these heterocyclic compounds play an important role in the field of Medicinal Chemistry. In fact, coumarins have been previously described as anticancer, antiviral, anti-inflammatory, antimicrobial, enzymatic inhibitory and antioxidant agents. Within the field of neurodegenerative diseases are described different types and intervention processes, which include the development of acetylcholinesterase (AChE) inhibitors, which combined with another drugs are used on therapy for Alzheimer's diseases. These inhibitors allow acetylcholine levels in the brain to stabilize or even enhance them, since it's established that this enzyme is responsible for the metabolism of this important neurotransmitter. In our group, we have already synthesised multiple novel compounds incorporating the coumarin moiety with remarkable activity towards MAO and/or AChE. In this work, we continue to exploit this scaffold by the synthesis of novel 3-amidocoumarins for the treatment of neurodegenerative diseases. Following this work, pharmacological studies of the prepared compounds as AChE inhibitors are currently in progress. Some preliminary results are presented in this communication.
Keywords: 3-amidocoumarins, Acetylcholinesterase inhibitors, Alzheimer's disease.