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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

Anti-inflammatory and Analgesic Activities of Edgeworthia chrysantha and Its Effective Chemical Constituents

TL;DR: It is demonstrated that the coumarins EdN, EdeA and EdeC in this plant may be active constituents that contribute to the anti-inflammatory and analgesic effects.
Journal ArticleDOI

Spectrofluorimetric method for the quantification of 7-hydroxycoumarin in urine and plasma using both extracted and unextracted samples

TL;DR: The percentage of the dose recovered as 7-OHC over a 24 h period was 92-98%, using unextracted and extracted samples, respectively, with 98% of this recovered as the glucuronide conjugate.
Journal ArticleDOI

Coumarins permeability in Caco-2 cell model.

TL;DR: This work evaluated the permeability and cytotoxicity of 18 coumarins, with different substitution patterns involving OH, OCH3 and CH3 groups, as a first event contributing to coumarin oral bioavailability.
Journal ArticleDOI

Substituted coumarins as esterase-sensitive prodrug moieties with improved release rates.

TL;DR: The synthesis and evaluation of several substituted coumarin-based prodrugs of model amines with significantly increased release rates are described.
Book ChapterDOI

4 Antihyperlipidaemic Agents

TL;DR: A survey of antihyperlipidaemic agents that are either in medical use or on trial, and some compounds exhibiting a close chemical relationship to these agents have also been discussed in this chapter.
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