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Synthesis and Study of a Selected Series of Amides with the Coumarin Scaffold for the Treatment of Alzheimer's Disease

Authors :
Lourdes Santana
Fernanda Borges
André Fonseca
Maria João Matos
Eugenio Uriarte
Yorley Duarte
Margarita Gutiérrez
Luis Astudillo
Source :
Proceedings of The 17th International Electronic Conference on Synthetic Organic Chemistry.
Publication Year :
2013
Publisher :
MDPI, 2013.

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.

Details

Database :
OpenAIRE
Journal :
Proceedings of The 17th International Electronic Conference on Synthetic Organic Chemistry
Accession number :
edsair.doi...........5ec4de2d44952fdba166bd17fefeacf8