Copper-catalyzed Convenient Synthesis and SAR Studies of Substituted-1,2,3-triazole as Antimicrobial Agents

Author(s): Aniket P. Sarkate*, Kshipra S. Karnik, Pravin S. Wakte, Ajinkya P. Sarkate, Ashwini V. Izankar, Devanand B. Shinde.

Journal Name: Letters in Drug Design & Discovery

Volume 16 , Issue 1 , 2019

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Graphical Abstract:


Background: A novel copper-catalyzed synthesis of substituted-1,2,3-triazole derivatives has been developed and performed by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The reaction is one-pot multicomponent.

Objective: We state the advancement and execution of a methodology allowing for the synthesis of some new substituted 1,2,3-triazole analogues with antimicrobial activity.

Methods: A series of triazole derivatives was synthesized by Huisgen 1,3-dipolar cycloaddition reaction of azides with alkynes. The structures of the synthesized compounds were elucidated and confirmed by 1H NMR, IR, MS and elemental analysis. All the synthesized compounds were tested for their antimicrobial activity against a series of strains of Bacillus subtilis, Staphylococcus aureus and Escherichia coli for antibacterial activity and against the strains of Candida albicans, Aspergillus flavus and Aspergillus nigar for antifungal activity, respectively.

Results and Conclusion: From the antimicrobial data, it was observed that all the newly synthesized compounds showed good to moderate level of antibacterial and antifungal activity.

Keywords: 1, 2, 3-triazole, copper, huisgen 1, 3-dipolar cycloaddition reaction, antibacterial, antifungal, antimicrobial.

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Year: 2019
Page: [3 - 10]
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DOI: 10.2174/1570180815666180326153322
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