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

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2018 Feb 1

PMID 29382051

Citations 127

Authors

Angela Stefanachi

Francesco Leonetti

Leonardo Pisani

Marco Catto

Angelo Carotti

Affiliations

Soon will be listed here.

Abstract

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.

Citing Articles

Playing Around the Coumarin Core in the Discovery of Multimodal Compounds Directed at Alzheimer's-Related Targets: A Recent Literature Overview.

Rullo M, La Spada G, Stefanachi A, Macchia E, Pisani L, Leonetti F Molecules. 2025; 30(4).

PMID: 40005200 PMC: 11857976. DOI: 10.3390/molecules30040891.

Zebrafish as a Suitable Model for Utilizing the Bioactivity of Coumarins and Coumarin-Based Compounds.

Lachowicz-Radulska J, Widelski J, Nowaczynski F, Serefko A, Sobczynski J, Ludwiczuk A Int J Mol Sci. 2025; 26(4).

PMID: 40003910 PMC: 11855297. DOI: 10.3390/ijms26041444.

Novel coumarin-based acetohydrazide-1,2,3-triazole derivatives as urease enzyme inhibitors: Synthesis, evaluation, and molecular dynamics simulation studies.

Sepehrmansourie H, Azimi M, Ebadi A, Chehardoli G, Zolfigol M, Amanlou M Heliyon. 2025; 11(1):e41321.

PMID: 39958735 PMC: 11825259. DOI: 10.1016/j.heliyon.2024.e41321.

Isolation and Identification of Coumarins from Citrus latifolia Leaves Using Advanced Chromatographic Techniques.

Fernandes H, Salome-Abarca L Methods Mol Biol. 2025; 2895:153-163.

PMID: 39885029 DOI: 10.1007/978-1-0716-4350-1_11.

α-Amylase inhibitory potential of dihydropyrano coumarins: In silico and DFT analysis.

Garg P, Bhatt H, Roy S, Reddy S 3 Biotech. 2025; 15(2):38.

PMID: 39807244 PMC: 11724822. DOI: 10.1007/s13205-024-04194-1.

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