A Comprehensive Review on Pharmacological Importance of Coumarin and Its Derivatives

Coumarins are a well-known group of naturally occurring benzopyrone compounds that are widely present in plants, microorganisms, and some marine environments, and they have gained significant importance as versatile frameworks in medicinal chemistry. Their basic structure, consisting of a fused benzene ring and an α-pyrone moiety, offers considerable flexibility for chemical modification, allowing the development of a wide variety of biologically active derivatives. In recent years, coumarins and their analogues have been extensively investigated due to their diverse pharmacological properties, such as antioxidant, antimicrobial, anti-inflammatory, anticoagulant, antiviral, antidiabetic, neuroprotective, and anticancer activities. These effects are mainly attributed to their ability to neutralize reactive oxygen species, inhibit key enzymes, regulate important cellular signaling pathways, and interact with nucleic acids, thereby contributing to their therapeutic potential in multiple disease conditions. Beyond their medicinal applications, coumarin derivatives also exhibit significant value in diagnostic and analytical fields because of their strong photophysical and fluorescent characteristics, which make them suitable for bioimaging, chemical sensing, and monitoring applications. Recent progress in synthetic chemistry, including eco-friendly methods, microwave-assisted synthesis, and multicomponent reactions, has enabled the efficient production of structurally diverse compounds with improved biological activity and selectivity. Moreover, the use of computational approaches such as molecular docking, quantitative structure–activity relationship analysis, and prediction of absorption, distribution, metabolism, excretion, and toxicity properties has facilitated the rapid identification and optimization of potential drug candidates. However, certain limitations, including low aqueous solubility, rapid metabolic breakdown, and potential toxicity, still pose challenges for their clinical use. Overall, coumarins continue to represent important and adaptable pharmacophores with promising prospects for the development of novel therapeutic and diagnostic agents in modern drug discovery.