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2000
Volume 1, Issue 1
  • ISSN: 2210-299X
  • E-ISSN: 2210-3007
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Abstract

Background

Tuberculosis (TB) is caused by and is one of the most contagious and fatal human pathogens which necessitates the development of modified existing drugs or derivatives with action against novel targets.

Aims and Objectives

In the present work, we have explored a few, 2-(5-(substituted)-4H-1,2,4-triazole-2-ylthio)-N-(substituted) phenyl acetamide (-) derivatives as anti-TB.

Materials and Methods

On the basis of SAR were synthesized and screened against H37Rv using MABA assay. Their ADME properties were also checked.

Results

ADME analysis showed results comparable with standard drug (rifampicin). Derivative turned out to be the most active amongst all the derivatives with MIC of 0.8μg/ml, comparable to standard drugs like rifampicin(0.8μg/ml) and streptomycin(0.8μg/ml).

Conclusion

All five compounds have shown excellent inhibitory activity (1.6µg/ml) against the H37Rv strain. Compound shows a promising activity (0.8µg/ml) as compared to standard drugs and also it has shown the highest docking score. Literature search has revealed the presence of 1,2,4-triazole derivatives linked to aromatic link and possessing amide linkage and the presence of Sulphur atom in the most active derivatives, which supports our designed compounds. Based on these findings, further derivatives would be synthesized and explored for their role in tuberculosis.

© 2023 The Author(s). Published by Bentham Science Publisher.
This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 International Public License (CC-BY 4.0), a copy of which is available at: https://creativecommons.org/licenses/by/4.0/legalcode. This license permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited.
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2023-01-01
2025-10-03

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ADME, Synthesis and Antimycobacterial Activity of 1,2,4-Triazol-3-thiol Linked Phenylacetamide Derivatives
Curr. Indian Sci. 1, E2210299X239429 (2023); https://doi.org/10.2174/012210299X239429231026060353
/content/journals/cis/10.2174/012210299X239429231026060353
/content/journals/cis/10.2174/012210299X239429231026060353
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  • Article Type:     Research Article
Keyword(s): ADME; Drugs; MABA; Mycobacterium tuberculosis H37Rv; Tuberculosis

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