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Letters in Organic Chemistry

Editor-in-Chief

ISSN (Print): 1570-1786
ISSN (Online): 1875-6255

Research Article

Phenyl Substituted Thiazole Linked 1, 2, 4-triazole Derivatives: Synthesis and Their Biological Evaluation

Author(s): Sonika Jain, Esha Dhall, Meenu Devi, Swapnil Sharma, Jaya Dwivedi and Sanjeev Kumar Sahu*

Volume 18, Issue 9, 2021

Published on: 06 November, 2020

Page: [727 - 734] Pages: 8

DOI: 10.2174/1570178617999201106113641

Price: $65

Abstract

Synthesize and evaluate some phenyl substituted thiazole linked 1, 2, 4-triazole derivatives as antimicrobial agents.

Compounds containing 1, 2, 4-triazole moieties are widely used as antimicrobial and antifungal agents whereas thiazole is another heterocyclic ring exhibiting various pharmacological actions. It is interesting to incorporate different bioactive pharmacophores in the same molecular framework to examine cumulative effect exerted by the moiety. This hypothesis was applied in research work by having triazole and thiazole in the same molecular framework.

The present work was mainly focused on synthesis of some 1, 2, 4-triazole derivatives linking with phenyl substituted thiazole nucleus and their evaluation for biological activity. The compounds (8a-8j) were synthesized as per design scheme and elucidated their structures using different spectroscopic data of IR, 1HNMR, 13CNMR & mass spectroscopy. These synthesized derivatives were evaluated for their antibacterial activity using broth dilution assay. Further, mechanism of action of test compounds was examined using protein leakage assay.

All the spectral data were confirmed the synthesis of phenyl substituted thiazole linked 1, 2, 4- triazole derivatives and some of them exhibited significant antimicrobial activity.

Amongst all compound 8c showed most potent activity with lowest IC50 values 180 μg/ml and 120 μg/ml against S. aureus & amp; B. cereus respectively. Whereas compound 8j demonstrated strong inhibitory activities only against negative strains P. aeruginosa and E. coli with lowest IC50 values 240 μg/mL and 200μg/mL respectively.

Keywords: Schiff bases, cyclizations, drug research, heterocycles, mass spectroscopy, antibacterial activity.

Graphical Abstract


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