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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 biological evaluation of novel benzimidazole derivatives and their binding behavior with bovine serum albumin.

TL;DR: Bioactive assay manifested that the bis-benzimidazole derivative 11d and its hydrochloride 13b exhibited remarkable antimicrobial activities, which were comparable or even better than the reference drugs Norfloxacin, Chloromycin and Fluconazole.
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Inhibitory effect of oxycoumarins isolated from the Thai medicinal plant Clausena guillauminii on the inflammation mediators, iNOS, TNF-α, and COX-2 expression in mouse macrophage RAW 264.7

TL;DR: Examination of the inhibitory effects of the known oxycoumarins poncitrin, osthol, and xanthoxyletin, newly isolated from Clausena guillauminii, revealed that the synthesis of nitric oxide (NO) and the protein expression of tumor necrosis factor-α and cyclooxygenase-2 (COX-2) were inhibited by 5.7 μM.
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Biological activity of chemical constituents from Clausena harmandiana.

TL;DR: The activity guided fractionation of the Clausena harmandiana root extracts led to the isolation of a coumarin, a ferulate, and eight carbazoles, which is the first report of the isolated of compounds 2–4 and 6–10 from this species.
Journal ArticleDOI

Anticonvulsant activity of furanocoumarins and the essential oil obtained from the fruits of Heracleum crenatifolium

TL;DR: The anticonvulsant activity of furanocoumarins, coumarin mixture and the essential oil obtained from the fruits of Heracleum crenatifolium was examined against maximal electroshock (MES)-induced seizures in mice as discussed by the authors.
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Synthesis and biological evaluation of hydroxylated 3-phenylcoumarins as antioxidants and antiproliferative agents

TL;DR: Interestingly, a new derivative, 6-methoxy-7-hydroxy-3-(4'-hydroxyphenyl)coumarin, 9, behaved as a poor antioxidant but appeared to be the most potent antiproliferative agent among the compounds examined, and this activity was mediated by deregulation in cell cycle and induction of apoptosis.
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