![]() This privileged scaffold serves as an important platform for the design of compound libraries in the search for new drug candidates. These compounds present a broad variety of applications, for example as photocleavable protecting groups or fluorescent probes. The luminescence of some derivatives results from the intrinsic charge transfer properties of electron-rich conjugated π-π systems. Despite being recognized for their biological activities, coumarins present another important characteristic widely explored by the industry: their luminescent properties. Moreover, some natural benzocoumarins show anti-algal activity. Their importance is also clear in the food industry where their fungicide and antioxidant activities are investigated and exploited. Coumarins exhibit several pharmacological effects including anticoagulant, antimicrobial, anti-inflammatory, neuroprotective, antidiabetic, anticonvulsant and antiproliferative. This review is intended to be a critical overview on coumarins, comprehensive of natural sources, metabolites, biological evaluations and synthetic approaches.Ĭoumarins have several attractive features, such as low molecular weight, simple structure, high bioavailability, high solubility in most of the organic solvents and low toxicity, which, together with their multifaceted biological activities, ensure them a prominent role as lead compounds in drug research and development. The versatility of coumarin scaffold finds applications not only in medicinal chemistry but also in the agrochemical field as well as in the cosmetic and fragrances industry. ![]() In addition, coumarin nucleus has proved to be easily synthetized and decorated, giving the possibility of designing new coumarin-based compounds and investigating their potential in the treatment of various diseases. In the last years, these natural compounds have been gaining an increasing attention from the scientific community for their wide range of biological activities, mainly due to their ability to interact with diverse enzymes and receptors in living organisms. ![]() Coumarin is a simple scaffold widespread in Nature and it can be found in a considerable number of plants as well as in some fungi and bacteria. Privileged structures have been widely used as an effective template for the research and discovery of high value chemicals. ![]()
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