A Review on Chalcones Synthesis and their Biological Activity

Verma, Shipra; Srivastava, Alok Kumar; Pandey, O. P.

doi:10.29161/pt.v6.i2.2018.22

Cited by 33 publications

(29 citation statements)

References 16 publications

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“…Sulfonylpiperazines linked with [1,3]dioxolo[4,5-g]chromenones (17) were synthesized by the aldol condensation and evaluated as antioxidants against DPPH, ABTS, as well as antiproliferative agents against non-cancer MDCK cell lines [21].…”

Section: Anticancer Chalconesmentioning

confidence: 99%

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Biological Role of Chalcones in Medicinal Chemistry

Tekale¹,

Mashele²,

Pooe³

et al. 2020

Vector-Borne Diseases - Recent Developments in Epidemiology and Control

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Chalcones are promising synthons and bioactive scaffolds of great medicinal interest due to their numerous pharmacological and biological activities. They are well recognized to possess antimicrobial, anticancer, antitubercular, antioxidant, anti-inflammatory, antileishmanial, and other significant biological activities. This chapter highlights recent updates and applications of chalcones as biologically, pharmacologically, and medicinally important entities.

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Section: Anticancer Chalconesmentioning

confidence: 99%

“…Chalcones constitute good synthons for a variety of novel heterocycles of high therapeutic potential and good pharmaceutical profile [1,2]. Chalcones themselves are identified as interesting entities associated with several biological activities [3].…”

Section: Introductionmentioning

confidence: 99%

Biological Role of Chalcones in Medicinal Chemistry

Tekale¹,

Mashele²,

Pooe³

et al. 2020

Vector-Borne Diseases - Recent Developments in Epidemiology and Control

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show abstract

“…Chalcones are related to the flavonoid family and generally found to be present in edible plants, polyphenolic compounds that exhibited yellow to orange color . Chalcones are the valuable synthones for the preparations of several synthetically and biologically potent heterocycles . Thus, syntheses of chalcones and pyrazolines have been widely exploited in the designing and developing the novel drugs .…”

Section: Introductionmentioning

confidence: 99%

New Biphenyl‐Based Bispyrazolines: Synthesis, Antimicrobial, and Docking Studies

Yusuf

Nisa

Paul

2019

Journal of Heterocyclic Chem

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In this study, a series of new bispyrazolines 8(a–f) have been prepared from the cyclization reactions of bischalcones 7(a–f) with phenyl hydrazine by refluxing under the alkaline alcoholic (KOH/EtOH) conditions. The O‐alkylation reactions of hydroxyl substituted chalcone 6 with different 1,ω‐dibromoalkanes in the presence of anhydrous potassium carbonate, tetrabutylammonium iodide, and dry acetone afforded the symmetrical new bischalcones 7(a–f) in good yields. Chalcone 6 was realized by using the Claisen–Schmidt reaction of m‐hydroxyacetophenone with bipheny‐4‐carboxaldehyde. The various spectroscopic parameters such as IR, 1H‐NMR, 13C‐NMR, and ESI‐MS have been thoroughly used for the structural interpretations of the newly prepared products. The in vitro antibacterial and antifungal activities of these compounds have been examined with the help of serial tube dilution method, and many of the tested products were found to be revealing the promising antimicrobial properties, which were evident from their minimum inhibitory concentration values. The molecular docking simulations of the synthesized substances have also been achieved to observe the structural association into the active site of the Escherichia coli FabH (PdB: 3IL9). Docking results of these compounds suggested that bispyrazoline 8b demonstrated the lowest binding energy that describes its higher stability into the pocket of E. coli. The excellent inhibitory activity of this bisheterocycle against E. coli FabH may be ascribed on the basis of hydrophobic and van der Waals interactions.

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“…Nitrogen and sulfurcontaining heterocyclic are an important class of heterocyclic compounds useful in medicinal chemistry [1][2][3] . Most of the five-membered nitrogen-containing heterocyclic are biologically active [4][5] . In the history of modern drug discovery, fused heterocyclic with Imidazothiazole moiety are interesting forthcoming objects.…”

Section: Introductionmentioning

confidence: 99%

Untitled

2019

IJPSR

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A series of condensed Imidazo [2, 1-b] [1,3] thiazole Chalcones have been synthesized by Claisen-Schmidt condensation reaction. Imidazo thiazole Chalcones are associated with immense biological activities. Novel Imidazo thiazole-based chalcones were synthesized using Imidazo thiazole-3carboxaldehydes and various acetyl ketones in PEG-400. The structures of the compounds were characterized by IR, 1 H NMR and screened for their in-vitro antioxidant (DPPH and SOD) activity. DPPH free radical scavenging activity was given by the compounds 7a-j at with (0.5 mmol/L in methanol). The compounds having substituent hydroxyl, fluoro, methoxy, ethoxy, and fluoro as well as benzimidazole and a ferrocenyl moiety in chalcone structure (7a-j) shows enhancement in antioxidant activity. Particularly in compounds like 7e, 7f, 7g, and 7h show the moderate percentage and 7c show the strongest percentage of inhibition mainly at (C=1mM). Almost all the compounds indicate moderate to good antioxidant activity compared to that of standard ascorbic acid percentage antioxidant activity (1 mm) by DPPH and SOD as 44.18 and 74.07 respectively. The resultant absorbance was recorded at 517 nm after 30 min incubation at 37 ºC. It was also found to be a potent scavenger of SOD, and this property may be responsible for the good anti-inflammatory activity of corresponding Imidazo-Thiazole Chalcones. Almost all the synthesized novel Imidazothiazole chalcones show potent antioxidant activity.

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A Review on Chalcones Synthesis and their Biological Activity

Cited by 33 publications

References 16 publications

Biological Role of Chalcones in Medicinal Chemistry

Biological Role of Chalcones in Medicinal Chemistry

New Biphenyl‐Based Bispyrazolines: Synthesis, Antimicrobial, and Docking Studies

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