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.
Highlights
This review is focused on the design, synthesis, bio-pharmacological evaluation, and data analysis of a large number of coumarin derivatives, mainly developed in our group, as monoamine oxidase (MAO), cholinesterase (ChE), and aromatase (AR) inhibitors, and as multitarget agents addressing neurodegenerative diseases (NDs)
Biotechnologies andcomparable, made commercially available, urged for possible correlations between activities determined on highly pure recombinant human MAO B with a set of known activities onMAO
Industrial interest on coumarins led to the development cosmetics, agrochemicals, polymeric
Summary
This review is focused on the design, synthesis, bio-pharmacological evaluation, and data analysis of a large number of coumarin derivatives, mainly developed in our group, as monoamine oxidase (MAO), cholinesterase (ChE), and aromatase (AR) inhibitors, and as multitarget agents addressing neurodegenerative diseases (NDs). A general overview of coumarins will be presented, followed by a discussion on the design, synthesis, and biological evaluation as enzyme inhibitors and multitarget ligands of suitably functionalized coumarins. Isolation, structural characterization, synthesis, and biological activity of thousands of natural coumarins from plants, bacteria, fungi [19,20,21], and chemical synthesis [22], have been reported. Coumarin 1, whose structure and numbering scheme are illustrated, is characterized by a 2H-chromen-2-one (1,2-benzopyrone, or 2H-1-benzopyran-2-one) oxa-heterocycle, and has been
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