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Synthesis and Study of a Selected Series of Amides with the Coumarin Scaffold for the Treatment of Alzheimer's Disease
Published: 31 October 2013 by MDPI in The 17th International Electronic Conference on Synthetic Organic Chemistry session Bioorganic, Medicinal and Natural Products
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.