Journal ArticleDOI
Recent advances and therapeutic journey of coumarins: current status and perspectives
Kuldipsinh P. Barot,Shailesh V. Jain,Laurent Kremer,Laurent Kremer,Shubhra Singh,Shubhra Singh,Shubhra Singh,Manjunath Ghate +7 more
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.read more
Citations
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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
Chemical feasibility studies of a potential coumarin-based prodrug system
TL;DR: In this paper, several amides of coumarinic acid with the phenolic hydroxyl group protected as an ester were prepared by using model amines, and these model amides underwent a facile ( t 1 2 1.5 −31 min) lactonization to release the original amine compounds upon esterase catalyzed hydrolysis of phenolic ester.
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Rapid and sensitive determination of coumarin and 7-hydroxycoumarin and its glucuronide conjugate in urine and plasma by high-performance liquid chromatography.
Denise A. Egan,Richard O'Kennedy +1 more
TL;DR: A rapid and sensitive high-performance liquid chromatographic method was developed for the analysis of coumarin, 7-hydroxycoumarin and its glucuronide conjugate in urine and plasma and includes an internal standard.
Journal ArticleDOI
Chalcone-based derivatives as new scaffolds for hA3 adenosine receptor antagonists.
Saleta Vazquez-Rodriguez,Maria João Matos,Maria João Matos,Lourdes Santana,Eugenio Uriarte,Fernanda Borges,Sonja Kachler,Karl-Norbert Klotz +7 more
TL;DR: The synthesis of a new series of coumarin–chalcone hybrids and the pharmacological characterization of their actions at four subtypes of AR are reported.
Journal ArticleDOI
Specific inhibition of cyclic amp-dependent protein kinase by warangalone and robustic acid
TL;DR: The selective, high affinity interaction of warangalone and robustic acid with cAK may contribute to their biological effects in vivo and to the insecticidal activity of the plant D. scandens.
Journal ArticleDOI
Two-year toxicity study on coumarin in the baboon.
J.G. Evans,I.F. Gaunt,B.G. Lake +2 more
TL;DR: Ulastructural examination of the liver revealed dilatation of the endoplasmic reticulum, a finding consistent with the early stages of intracellular oedema in hepatocytes, in three of the four animals fed 67·5 mg coumarin/kg/day, and a significant increase in liver weight expressed relative to body weight was recorded in this group.
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