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Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds
Many naturally occurring substances, traditionally used in popular medicines around the world, contain the coumarin moiety. Coumarin represents a privileged scaffold for medicinal chemists, because of its peculiar physicochemical features, and the versatile and easy synthetic transformation into a l...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2018
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017103/ https://www.ncbi.nlm.nih.gov/pubmed/29382051 http://dx.doi.org/10.3390/molecules23020250 |
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author | Stefanachi, Angela Leonetti, Francesco Pisani, Leonardo Catto, Marco Carotti, Angelo |
author_facet | Stefanachi, Angela Leonetti, Francesco Pisani, Leonardo Catto, Marco Carotti, Angelo |
author_sort | Stefanachi, Angela |
collection | PubMed |
description | Many naturally occurring substances, traditionally used in popular medicines around the world, contain the coumarin moiety. Coumarin represents a privileged scaffold for medicinal chemists, because of its peculiar physicochemical features, and the versatile and easy synthetic transformation into a large variety of functionalized coumarins. As a consequence, a huge number of coumarin derivatives have been designed, synthesized, and tested to address many pharmacological targets in a selective way, e.g., selective enzyme inhibitors, and more recently, a number of selected targets (multitarget ligands) involved in multifactorial diseases, such as Alzheimer’s and Parkinson’s diseases. In this review an overview of the most recent synthetic pathways leading to mono- and polyfunctionalized coumarins will be presented, along with the main biological pathways of their biosynthesis and metabolic transformations. The many existing and recent reviews in the field prompted us to make some drastic selections, and therefore, the review is focused on monoamine oxidase, cholinesterase, and aromatase inhibitors, and on multitarget coumarins acting on selected targets of neurodegenerative diseases. |
format | Online Article Text |
id | pubmed-6017103 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2018 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-60171032018-11-13 Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds Stefanachi, Angela Leonetti, Francesco Pisani, Leonardo Catto, Marco Carotti, Angelo Molecules Review Many naturally occurring substances, traditionally used in popular medicines around the world, contain the coumarin moiety. Coumarin represents a privileged scaffold for medicinal chemists, because of its peculiar physicochemical features, and the versatile and easy synthetic transformation into a large variety of functionalized coumarins. As a consequence, a huge number of coumarin derivatives have been designed, synthesized, and tested to address many pharmacological targets in a selective way, e.g., selective enzyme inhibitors, and more recently, a number of selected targets (multitarget ligands) involved in multifactorial diseases, such as Alzheimer’s and Parkinson’s diseases. In this review an overview of the most recent synthetic pathways leading to mono- and polyfunctionalized coumarins will be presented, along with the main biological pathways of their biosynthesis and metabolic transformations. The many existing and recent reviews in the field prompted us to make some drastic selections, and therefore, the review is focused on monoamine oxidase, cholinesterase, and aromatase inhibitors, and on multitarget coumarins acting on selected targets of neurodegenerative diseases. MDPI 2018-01-27 /pmc/articles/PMC6017103/ /pubmed/29382051 http://dx.doi.org/10.3390/molecules23020250 Text en © 2018 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Stefanachi, Angela Leonetti, Francesco Pisani, Leonardo Catto, Marco Carotti, Angelo Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds |
title | Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds |
title_full | Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds |
title_fullStr | Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds |
title_full_unstemmed | Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds |
title_short | Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds |
title_sort | coumarin: a natural, privileged and versatile scaffold for bioactive compounds |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6017103/ https://www.ncbi.nlm.nih.gov/pubmed/29382051 http://dx.doi.org/10.3390/molecules23020250 |
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