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Research Article

Synthesis, Antimicrobial Evaluation and Docking Study of Novel Thiosemicarbazone Clubbed with 1,2,3-Triazoles

Author(s): Adinath D. Badar, Shubham M. Sulakhe, Mahesh B. Muluk, Naziya N. M. A. Rehman, Prashant P. Dixit, Prafulla B. Choudhari, Giribala M. Bondle and Kishan P. Haval*

Volume 17, Issue 6, 2021

Published on: 11 September, 2020

Article ID: e010621185856 Pages: 10

DOI: 10.2174/1573407216999200911121853

Price: $65

Abstract

Background: Thiosemicarbazone, 1,2,3-triazole and their derivatives received great pharmaceutical importance due to their prominent biological activities. In the present study, the molecular hybrid thiosemicarbazone-1,2,3-triazoles derivatives were synthesized and screened for their antimicrobial activities.

Methods: A series of thiosemicarbazone clubbed with 1,2,3-triazole derivatives were synthesized via click chemistry approach in good yields. The structures of synthesized compounds were assigned by their spectral data. The in vitro antimicrobial activity was performed by the agar well diffusion method. A molecular docking study was performed to identify the possible mode of action of synthesized derivatives.

Results: The compounds 5d, 5h, 5i and 5k exhibited excellent antimicrobial activities against both antibacterial and antifungal pathogens. The active thiosemicarbazone-1,2,3-triazole derivatives showed excellent binding affinity towards DNA gyrase.

Conclusion: The molecular hybrid thiosemicarbazone-1,2,3-triazole derivatives were synthesized. The newly synthesized compounds were evaluated for their antimicrobial activities. Few of the thiosemicarbazone-1,2,3-triazoles derivatives have exhibited good antimicrobial activities. They have shown excellent binding affinity towards DNA gyrase.

Keywords: 1, 2, 3-triazole, thiosemicarbazone, antimicrobial Activity, molecular Docking Study, click Chemistry.

Graphical Abstract

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