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Abstract <p>Coumarins, a class of benzopyran-derived compounds, have emerged as versatile bioorganic building blocks with significant roles in drug design, biocatalysis, and sensing applications. These naturally occurring and synthetically derived molecules exhibit a wide range of biological activities, including antimicrobial, anti-inflammatory, anticancer, and anticoagulant properties. Due to the diversity of hydroxyl, methoxy, and prenyl substitutions, coumarins can adopt various structures, enabling functionalization for a broad spectrum of biomedical and industrial uses. In the field of drug discovery, coumarins have been extensively studied as enzyme inhibitors, fluorescence probes, and molecular scaffolds for novel therapeutics. Their ability to form both covalent and non-covalent interactions with biological targets makes them promising candidates for pharmaceutical development. Due to their unique photophysical properties, coumarins can also serve as molecular sensors for detecting metal ions, reactive oxygen species, and biomolecules in living systems. Biocatalysis has also benefited from the incorporation of coumarins, as they act as substrates and modulators in enzyme-mediated transformations. Enzymatic pathways for coumarin biosynthesis and functionalization have been explored to improve their accessibility and biocompatibility. Recent advances in biotechnological approaches, such as metabolic engineering and microbial synthesis, have further facilitated the production of complex coumarin derivatives with tailored bioactivities. Furthermore, coumarins play a key role in the development of optical and electrochemical sensors due to their tunable fluorescence and electron transfer properties. They have been employed in environmental monitoring, disease diagnostics, and chemical safety assessments, demonstrating their broad applicability beyond medicinal chemistry. Despite their promising potential, challenges such as bioavailability, toxicity, and regulatory constraints must be addressed to optimize their therapeutic and industrial utility. This review comprehensively examines the chemical, biological, and functional aspects of coumarins in bioorganic chemistry, highlighting their significance in modern scientific and technological advancements. By integrating recent findings and emerging trends, this article aims to provide insights into the future directions and innovations in coumarin-based research.</p>

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Coumarins as Bioorganic Building Blocks in Drug Design, Biocatalysis, and Sensing

  • 期刊论文

  • 发表日期：

    2025年12月1日

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  • Yasser Fakri Mustafa

摘要

Abstract

Coumarins, a class of benzopyran-derived compounds, have emerged as versatile bioorganic building blocks with significant roles in drug design, biocatalysis, and sensing applications. These naturally occurring and synthetically derived molecules exhibit a wide range of biological activities, including antimicrobial, anti-inflammatory, anticancer, and anticoagulant properties. Due to the diversity of hydroxyl, methoxy, and prenyl substitutions, coumarins can adopt various structures, enabling functionalization for a broad spectrum of biomedical and industrial uses. In the field of drug discovery, coumarins have been extensively studied as enzyme inhibitors, fluorescence probes, and molecular scaffolds for novel therapeutics. Their ability to form both covalent and non-covalent interactions with biological targets makes them promising candidates for pharmaceutical development. Due to their unique photophysical properties, coumarins can also serve as molecular sensors for detecting metal ions, reactive oxygen species, and biomolecules in living systems. Biocatalysis has also benefited from the incorporation of coumarins, as they act as substrates and modulators in enzyme-mediated transformations. Enzymatic pathways for coumarin biosynthesis and functionalization have been explored to improve their accessibility and biocompatibility. Recent advances in biotechnological approaches, such as metabolic engineering and microbial synthesis, have further facilitated the production of complex coumarin derivatives with tailored bioactivities. Furthermore, coumarins play a key role in the development of optical and electrochemical sensors due to their tunable fluorescence and electron transfer properties. They have been employed in environmental monitoring, disease diagnostics, and chemical safety assessments, demonstrating their broad applicability beyond medicinal chemistry. Despite their promising potential, challenges such as bioavailability, toxicity, and regulatory constraints must be addressed to optimize their therapeutic and industrial utility. This review comprehensively examines the chemical, biological, and functional aspects of coumarins in bioorganic chemistry, highlighting their significance in modern scientific and technological advancements. By integrating recent findings and emerging trends, this article aims to provide insights into the future directions and innovations in coumarin-based research.