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

Area of Science:

• Medicinal Chemistry
• Organic Synthesis
• Pharmacology

Background:

• Coumarin derivatives are prevalent in natural products and traditional medicines.
• The coumarin scaffold offers unique physicochemical properties and synthetic versatility.
• Numerous coumarin derivatives have been developed as selective pharmacological agents.

Purpose of the Study:

• To review recent synthetic pathways for functionalized coumarins.
• To explore the biosynthesis and metabolic transformations of coumarins.
• To focus on coumarin derivatives as inhibitors of specific enzymes and multitarget ligands for neurodegenerative diseases.

Main Methods:

• Literature review of recent synthetic strategies for coumarins.
• Analysis of biological data on coumarin derivatives.
• Focus on enzyme inhibition (monoamine oxidase, cholinesterase, aromatase) and multitarget applications.

Main Results:

• Overview of novel synthetic routes to mono- and polyfunctionalized coumarins.
• Discussion of coumarin biosynthesis and metabolism.
• Identification of coumarins targeting key enzymes and pathways in neurodegenerative diseases.

Conclusions:

• Coumarins are privileged scaffolds with broad therapeutic potential.
• Recent synthetic advancements enable diverse coumarin derivative development.
• Coumarins show promise as inhibitors and multitarget agents for complex diseases like Alzheimer's and Parkinson's.