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Journal ArticleDOI

Recent advances and therapeutic journey of coumarins: current status and perspectives

TLDR
The occurence, synthesis and specific biological activities of various coumarin derivatives are described for the discovery and development of new synthetic strategies that could help in structure–activity relationship (SAR) studies.
Abstract
Coumarins are oxygen-containing molecules with specific benzopyrone nucleus. Different coumarins are identified as antineurodegeneratives, anticoagulants, antioxidants, antimicrobials, anticancers, antivirals, antidiabetics, antidepressants, supramoleculars, antiparasitics, anti-inflammatory, analgesics, biological stains, pathological probes and diagnostics. Coumarins have received more attention as compared to 1-azacoumarins. Many attempts have been made for the comparison of both the systems at different stages to discover novel synthetic methodologies, reactivity strategies and biological activities. Translation of current knowledge into novel potent lead compounds and repositioning of well-known compounds for the treatment of different acute and chronic diseases are the current challenges of coumarins. This review article focusses on the occurence, synthesis and specific biological activities of various coumarin derivatives. Some novel research approaches are also described for the discovery and development of new synthetic strategies that could help in structure–activity relationship (SAR) studies. Cellular and molecular mechanisms of coumarins involved in SAR studies are also described.

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Reactive oxygen species

Journal ArticleDOI

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

TL;DR: An overview of the most recent synthetic pathways leading to mono- and polyfunctionalized coumarins will be presented, along with the main biological pathways of their biosynthesis and metabolic transformations.
Journal ArticleDOI

An overview of coumarin as a versatile and readily accessible scaffold with broad-ranging biological activities

TL;DR: This review is intended to be a critical overview on coumarins, comprehensive of natural sources, metabolites, biological evaluations and synthetic approaches.
Journal ArticleDOI

New Insights into the Antibacterial Activity of Hydroxycoumarins against Ralstonia solanacearum

TL;DR: It is demonstrated that hydroxycoumarins have superior antibacterial activity against the phytopathogen R. solanacearum, and thus have the potential to be applied for controlling plant bacterial wilt.
Journal ArticleDOI

Synthesis of novel coumarin appended bis(formylpyrazole) derivatives: Studies on their antimicrobial and antioxidant activities.

TL;DR: Detailed quantitative structure-activity relationship (QSAR) analysis indicated the molecular parameters that contribute to increased potency of inhibition and would further encourage understanding in employing coumarin pyrazole hybrids as potential antibiotic agents for treating infections caused by pathogenic microbes and fungi.
References
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Journal ArticleDOI

The effect of alkylation on the antimicrobial activities of 7-hydroxy- and 4-hydroxycoumarins.

TL;DR: Es wird der Einfluss einer Alkylierung auf die antimikrobielle Wirkung von 7-hydroxy- und 4-Hydroxy-Cumarin dargestellt.
Journal ArticleDOI

The coumarin osthol attenuates the binding of thyrotropin-releasing hormone in rat pituitary GH4C1 cells.

TL;DR: Osthol modulates TRH-evoked responses by interacting with the TRH receptor and decreases the uptake of 45Ca2+ in response to high K+.
Journal ArticleDOI

The effect of substitution patterns on the release rates of opioid peptides DADLE and [Leu5]-enkephalin from coumarin prodrug moieties

TL;DR: Aimed at further understanding the structure-release rate relationship of the coumarin-based cyclic prodrugs, a series of substituted coumarinic acid derivatives of opioid peptides, DADLE, and [Leu(5)]-enkephalin are synthesized and examined.
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