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
Mechanism of biochemical action of substituted 4-methylbenzopyran-2-ones. Part I: Dioxygenated 4-methyl coumarins as superb antioxidant and radical scavenging agents.
Hanumantharao G. Raj,Virinder S. Parmar,Subhash C. Jain,Sanjay Goel,Poonam Himanshu,Sanjay Malhotra,Amarjit Singh,Carl Erik Olsen,Jesper Wengel +8 more
TL;DR: Seven 4-methylcoumarins bearing different functionalities have been examined for the first time for their effect on NADPH-catalysed liver-microsomal lipid peroxidation and 7,8-dihydroxy- and diacetoxy-4-methylCoumarin were found to possess superb antioxidant and radical scavenging activities.
Journal ArticleDOI
Mechanism of biochemical action of substituted 4-methylcoumarins. Part 11: Comparison of the specificities of acetoxy derivatives of 4-methylcoumarin and 4-phenylcoumarin to acetoxycoumarins: protein transacetylase.
Ajit Kumar,Brajendra K. Singh,Rahul Tyagi,Rahul Tyagi,Sapan K. Jain,Sunil K. Sharma,Sunil K. Sharma,Ashok K. Prasad,Hanumantharao G. Raj,Ramesh C. Rastogi,Arthur C. Watterson,Virinder S. Parmar,Virinder S. Parmar +12 more
TL;DR: It is demonstrated that the acetoxy coumarins and acetoxy dihydrocoumarins having a methyl group instead of a phenyl ring at the C-4, when used as the substrates, resulted in enhancement of TAase activity, while the saturation of double bond at C-3 and C- 4 position had no effect on TA enzyme activity.
Journal ArticleDOI
Inhibitory Effects of Coumarins from the Stem Barks of Fraxinus rhynchophylla on Adipocyte Differentiation in 3T3-L1 Cells
TL;DR: Results suggest that esculetin (1), an active compound from F. rhynchophylla, inhibited early stage of adipogenic differentiation, in part, via inhibition of PPARgamma-dependent pathway.
Journal ArticleDOI
A novel dimeric coumarin analog and antimycobacterial constituents from Fatoua pilosa.
TL;DR: One novel dimeric coumarin analog, fatouapilosin, together with 18 known compounds, have been isolated from the whole plants of Fatoua pilosa and exhibited the strongest antimycobacterial activities against Mycobacterium tuberculosis H37Rv.
Journal ArticleDOI
Synthesis and molecular docking study of novel coumarin derivatives containing 4,5-dihydropyrazole moiety as potential antitumor agents.
Xin-Hua Liu,Hui-Feng Liu,Jin Chen,Yang Yang,Baoan Song,Lin-Shan bai,Jing-Xin Liu,Zhu Hailiang,Zhu Hailiang,Xing-Bao Qi +9 more
TL;DR: A series of novel coumarin derivatives containing 4,5-dihydropyrazole moiety as potential telomerase inhibitors were synthesized and bioassay tests show that compound 3d exhibited potentially high activity against human gastric cancer cell SGC-7901.
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