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Molecules 2018, 23(2), 250; doi:10.3390/molecules23020250

Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds

Dipartimento di Farmacia-Scienze del Farmaco, Università degli Studi di Bari “Aldo Moro”, via E. Orabona 4, I-70125 Bari, Italy
Author to whom correspondence should be addressed.
Received: 19 December 2017 / Revised: 22 January 2018 / Accepted: 25 January 2018 / Published: 27 January 2018
(This article belongs to the Special Issue Versatile Coumarins)


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. View Full-Text
Keywords: coumarin; aromatase inhibitors; cholinesterase inhibitors; monoamine oxidase inhibitors; multitarget ligands coumarin; aromatase inhibitors; cholinesterase inhibitors; monoamine oxidase inhibitors; multitarget ligands

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Stefanachi, A.; Leonetti, F.; Pisani, L.; Catto, M.; Carotti, A. Coumarin: A Natural, Privileged and Versatile Scaffold for Bioactive Compounds. Molecules 2018, 23, 250.

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