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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

Synthesis and evaluation of novel substituted 5-hydroxycoumarin and pyranocoumarin derivatives exhibiting significant antiproliferative activity against breast cancer cell lines.

TL;DR: The results showed that compounds such as 6b, 6d, 6h, and 6k possess significant antiproliferative activity against MCF-7 cell line with the IC(50) values of 7.2, 5.3, 3.5 microM, respectively.
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Determination of free and total 7-hydroxycoumarin in urine and serum by capillary electrophoresis.

TL;DR: The CE method was found to decrease the analysis time in comparison to HPLC analysis, with results available after 1.5 min as compared to 12 min with HPLC, and there was no statistical difference between the results determined by either method.
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Acetoxy drug: protein transacetylase of buffalo liver-characterization and mass spectrometry of the acetylated protein product.

TL;DR: The purification and characterization of the buffalo liver microsomal transacetylase (TAase) catalyzing the transfer of acetyl groups from a model acetoxy drug to GST3-3 and the identity of the seven acetylated GST tryptic peptides could be confirmed by the application of LC/MS/MS.
Journal ArticleDOI

Metabolism and toxicity of coumarin on cultured human, rat, mouse and rabbit hepatocytes

TL;DR: The rat may not be a suitable model for evaluating the pharmacological hazards of coumarin in humans, and interspecies comparisons showed that rat hepatocytes were the most sensitive to the toxicity of cou marin and its derivatives, whereas human hepatocyteswere the most resistant.
Journal ArticleDOI

On the properties of Calcein Blue.

TL;DR: Calcein Blue, although satisfactory as an indicator, is not useful for the direct fluorometric determination of calcium, because the calcium derivative is changed on standing in highly alkaline solution to another fluorescent material.
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