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Green ultrasound-assisted three-component click synthesis of novel 1H-1,2,3-triazole carrying benzothiazoles and fluorinated-1,2,4-triazole conjugates and their antimicrobial evaluation.

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TLDR
An efficient and ecofriendly, ultrasound, one-pot click cycloaddition approach for the construction of a novel series of 1,4-disubstituted-1,2,3-triazoles tethered with fluorinated 1,2-4-Triazole-benzothiazole molecular conjugates, recognized for their antimicrobial activity against some bacterial and fungal pathogenic strains.
Abstract
The present study describes an efficient and ecofriendly, ultrasound, one-pot click cycloaddition approach for the construction of a novel series of 1,4-disubstituted-1,2,3-triazoles tethered with fluorinated 1,2,4-triazole-benzothiazole molecular conjugates. It involved three-component condensation of the appropriate bromoacetamide benzothiazole, sodium azide and 4-alkyl/aryl-5-(2-fluorophenyl)-3-(prop-2-ynylthio)-1,2,4-triazoles 4a-e through a Cu(I)-catalyzed 1,3-dipolar cycloaddition reaction. This approach involves in situ generation of azidoacetamide benzothiazole, followed by condensation with terminal alkynes in the presence of CuSO4/Na-ascorbate in aqueous DMSO under both conventional and ultrasound conditions. Some of the designed 1,2,3-triazole conjugates 6a-o were recognized for their antimicrobial activity against some bacterial and fungal pathogenic strains.

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Journal ArticleDOI

Design, synthesis, DNA binding, modeling, anticancer studies and DFT calculations of Schiff bases tethering benzothiazole-1,2,3-triazole conjugates

TL;DR: In this paper, focused thiopropargylated benzothiazole was reacted with ethyl azidoacetate and/or ethyl Azidobenzoate to yield newer 1,2,3-triazole-benzothiazoles conjugates bearing ester functionality through click chemistry approach.
Journal ArticleDOI

Design, Synthesis and Anticancer Screening of Novel Benzothiazole-Piperazine-1,2,3-Triazole Hybrids

TL;DR: A library of novel regioselective 1,4,5-trisubstituted-1,2,3-triazole based benzothiazole-piperazine conjugates designed and synthesized using the click synthesis approach in the presence and absence of the Cu(I) catalyst found good agreement with in vitro activity.
References
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Journal ArticleDOI

Efficient Conversion of Aromatic Amines into Azides: A One-Pot Synthesis of Triazole Linkages

TL;DR: An efficient and improved procedure for the preparation of aromatic azides and their application in the Cu(I)-catalyzed azide-alkyne 1,3-dipolar cycloaddition ("click reaction") is described.
Journal ArticleDOI

Isavuconazole: A New Broad-Spectrum Triazole Antifungal Agent

TL;DR: A randomized, double-blind comparison clinical trial for treatment of invasive aspergillosis found that the efficacy of isavuconazole was noninferior to that of voriconazole.
Journal ArticleDOI

2,4-Dihydro-3H-1,2,4-triazole-3-thiones as potential antidepressant agents.

TL;DR: One member of this series, compound 22, was selected for further evaluation in an electrophysiological model where it was found to reduce norepinephrine function in the cerebellum as measured by the NE augmentation of GABA inhibition of Purkinje neurons.
Journal ArticleDOI

1,2,3-Triazole derivatives as antitubercular agents: synthesis, biological evaluation and molecular docking study

TL;DR: Based on the results from the anti-tubercular activity, SAR for the synthesized series has been developed and this series is considered as a starting point for the development of novel and more potent anti-Tubercular agents in the future.
Journal ArticleDOI

Supported protic acid-catalyzed synthesis of 2,3-disubstituted thiazolidin-4-ones: enhancement of the catalytic potential of protic acid by adsorption on solid supports

TL;DR: In this article, the catalytic potential of various protic acids has been assessed for the one pot tandem condensation-cyclisation reaction involving an aldehyde, an amine, and thioglycolic acid to form 2,3-disubstituted thiazolidin-4-ones.
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