Design, synthesis, characterization, antimicrobial evaluation and molecular modeling studies of some dehydroacetic acid-chalcone-1,2,3-triazole hybrids

Lal, Kashmiri; Yadav, Pinki; Kumar, Ashwani; Kumar, Anil; Paul, Avijit Kumar

doi:10.1016/j.bioorg.2018.01.016

Cited by 121 publications

(64 citation statements)

References 49 publications

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“…In this regard, a set of 1,2,3-triazole-linked dehydroacetic acid-chalcone derivatives were synthesised for antimicrobial evaluation. 89 The hybrid compounds containing a substituted benzene portion exhibited more promising activity than dehydroacetic acid and dehydroacetic acid-chalcone alkyne. Among them, derivative 52 ( Fig.…”

Section: Antimicrobial Activitymentioning

confidence: 97%

1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview

Bozorov

Zhao

Aisa

2019

Bioorganic & Medicinal Chemistry

575

289

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A B S T R A C TThe 1,2,3-triazole ring is a major pharmacophore system among nitrogen-containing heterocycles. These fivemembered heterocyclic motifs with three nitrogen heteroatoms can be prepared easily using 'click' chemistry with copper-or ruthenium-catalysed azide-alkyne cycloaddition reactions. Recently, the 'linker' property of 1,2,3-triazoles was demonstrated, and a novel class of 1,2,3-triazole-containing hybrids and conjugates was synthesised and evaluated as lead compounds for diverse biological targets. These lead compounds have been demonstrated as anticancer, antimicrobial, anti-tubercular, antiviral, antidiabetic, antimalarial, anti-leishmanial, and neuroprotective agents. The present review summarises advances in lead compounds of 1,2,3-triazolecontaining hybrids, conjugates, and their related heterocycles in medicinal chemistry published in 2018. This review will be useful to scientists in research fields of organic synthesis, medicinal chemistry, phytochemistry, and pharmacology. Chemistry: synthesis and properties of the 1,2,3-triazolesThe general synthetic route of 1,2,3-triazoles using click chemistry is described in Scheme 1A. The most popular route to 1,2,3-triazoles is Cu(I)-catalysed Huisgen 1,3-dipolar cycloaddition, which is the https://doi.

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Section: Antimicrobial Activitymentioning

confidence: 97%

1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview

Bozorov

Zhao

Aisa

2019

Bioorganic & Medicinal Chemistry

575

289

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“…However, much of the pharmacological potential of chalcones and their recent updates need to be understood. The purpose of this chapter is to cover and describe the recent developments, preferably after 2015 to date, the utility of chalcones as medicinally Dehydroacetic acid chalcone-1,2,3-triazole hybrids (5) were shown to possess good in vitro antimicrobial activities against Staphylococcus epidermidis, Bacillus subtilis, Escherichia coli, and Pseudomonas aeruginosa bacteria and two fungal strains, viz., Aspergillus niger and Candida albicans [11].…”

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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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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“…Literature revealed that some molecular hybrid compounds having broad spectrum of biological activities (Fig. ) .…”

Section: Introductionmentioning

confidence: 99%

Synthesis, antimicrobial activity, and molecular docking study of formylnaphthalenyloxymethyl‐triazolyl‐N‐phenylacetamides

Muluk

Dhumal

Phatak

et al. 2019

Journal of Heterocyclic Chem

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In the present study, substituted formylnaphthalenyloxymethyl‐triazolyl‐N‐phenylacetamide derivatives (6a–k) have been designed and synthesized employing click chemistry approach and evaluated for their in vitro antifungal and antibacterial activities. All the newly synthesized compounds were thoroughly characterized by 1H NMR, 13C NMR, and HRMS spectral techniques. Among the screened compounds, 6d, 6e, 6j, and 6k have shown good antifungal and antibacterial activities. Compound 6k has shown very effective antimicrobial activity. We further performed exploratory docking studies on microbial DNA gyrase to rationalize the in vitro biological data and to demonstrate the mechanism of antimicrobial activity. This is the first report to demonstrate the formylnaphthalenyloxymethyl, triazole, and N‐phenylacetamide hybrids as potential antimicrobial agents.

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Design, synthesis, characterization, antimicrobial evaluation and molecular modeling studies of some dehydroacetic acid-chalcone-1,2,3-triazole hybrids

Cited by 121 publications

References 49 publications

1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview

1,2,3-Triazole-containing hybrids as leads in medicinal chemistry: A recent overview

Biological Role of Chalcones in Medicinal Chemistry

Synthesis, antimicrobial activity, and molecular docking study of formylnaphthalenyloxymethyl‐triazolyl‐N‐phenylacetamides

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