Therapeutic Journey and Recent Advances in the Synthesis of Coumarin Derivatives

Abstract

Background: Coumarin is an oxygen-containing compound in medicinal chemistry. Coumarin plays an important role in both natural systems like plants and also in synthetic medicinal applications as drug molecules. Many structurally different coumarin compounds were found to show a big range of similarity with the vital molecular targets for their pharmacological action and small modifications in their structures resulted insignificant changes in their biological activities. Objective: This review gives detailed information about the studies of the recent advances in various pharmacological aspects of coumarins. Method: Various oxygen-containing heterocyclic compounds represented remarkable biological significances. The fused aromatic oxygen-heterocyclic nucleus is able to change its electron density; thus changing the chemical, physical and biological properties respectively due to its multiple binding modes with the receptors, which play crucial role in pharmacological screening of drugs. A number of heterocyclic compounds have been synthesized which have their nucleus derived from various plants and animals. In coumarins, benzene ring is fused with pyrone nucleus which provides stability to the nucleus. Coumarins have shown a wide range of pharmacological activities such as anti-tumour, anti-coagulant, anti-inflammatory, anti-oxidant, antiviral, anti-malarial, anti-HIV and antimicrobial activity etc. Results: Reactive oxygen species like superoxide anion, hydroxyl radical and hydrogen peroxide are a type of unstable molecule that contains oxygen, which reacts with other molecules in the cell during the metabolism process but it may produce cytotoxicity when reactive oxygen species increase in number, by the damage of biological macromolecules. Hydroxyl radical (˙OH), is a strong oxidizing agent and it is responsible for the cytotoxicity by oxygen in different plants, animals and other microbes. coumarin is the oldest and effective compound having antimicrobial activity, anti-inflammatory, antioxidant, antidepressant activity, analgesic, anticonvulsant activity, etc. Naturally existing coumarin compounds act against SARS-CoV-2 by preventing viral replication through the targeting on active site against the Mpro target protein. Conclusion: This review highlights the different biological activities of coumarin derivatives. In this review we provide an updated summary of the researches which are related to recent advances in biological activities of coumarins analogue and their most recent activities against COVID -19. Natural compounds act as a rich resource for novel drug development against various SARS-CoV-2 viral strains including viruses like herpes simplex virus, influenza virus, human immunodeficiency virus, hepatitis B and C viruses, middle east respiratory syndrome and severe acute respiratory syndrome.

Cytogenotoxicity assessment of 3‐(3,4‐dihydroxyphenyl)‐7,8‐dihydroxycoumarin on HepG2/C3A cells and leukocytes

“…Coumarins are found mainly in fruits and flowers, and also in other sources, as olive oil, coffee, wine, black or green tea, citrus fruits, cinnamon, and essential oils such as cinnamon bark and lavender oils (Heghes et al, 2022; Matos et al, 2015). The simplicity of the coumarins' chemical structure, the synthetic accessibility, and the substitution variability of these heterocyclic compounds allow these molecules to display a huge range of pharmacological properties (Pisano et al, 2019; Sinha et al, 2022). These properties depend on the substitution patterns and allow several therapeutic applications, increasing the interest of these derivatives as phytochemicals (Carneiro et al, 2021; Matos et al, 2015).…”

“…huge range of pharmacological properties (Pisano et al, 2019;Sinha et al, 2022). These properties depend on the substitution patterns and allow several therapeutic applications, increasing the interest of these derivatives as phytochemicals (Carneiro et al, 2021;Matos et al, 2015).…”

Examining the Antioxidant and Superoxide Radical Scavenging Activity of Anise, (Pimpinella anisum L. Seeds), Esculetin, and 4-Methyl-Esculetin Using X-ray Diffraction, Hydrodynamic Voltammetry and DFT Methods

“…The interesting and varied chemical nature of coumarin derivatives and how these derivatives correlate with pharmacological and medicinal properties has been reported in several foundational reviews [ 16 , 43 , 44 , 45 , 46 , 47 ]. Current reviews that describe coumarin scavenging of superoxide include references [ 48 , 49 ]. In addition, the antioxidant abilities of coumarin metal complexes to scavenge free radicals recently has been reported in an excellent review [ 50 ].…”

Pharmacological activities of esculin and esculetin: A review

“…[ 2 ] Coumarins (1-benzopyran-2-one) are natural compounds of the benzopyrone class that are widely distributed in plants, as well as many species of fungi and bacteria. [ 3 ] Various promising pharmacological activities of coumarins were reported by many in vivo and in vitro studies, including anti-inflammatory, [ 4 ] antioxidant, [ 5 ] antibacterial, [ 6 ] anti-tumor, [ 7 ] and so on. As natural products, coumarins are considered promising as complementary and alternative medicines.…”