SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 4-((SUBSTITUTED BENZYLIDENE)AMINO)-5-(PYRIDIN-4-YL)-4H-1,2,4-TRIAZOLE-3-THIOL DERIVATIVES AS POTENTIAL ANTICANCER, ANTIMICROBIAL AND ANTI-INFLAMMATORY AGENTS

The anticancer, antimicrobial and anti-inflammatory properties of a novel series of 4-((substituted benzylidene)amino)-5-(pyridin-4-yl)-4H-1,2,4-triazole-3-thiol derivatives were synthesized and analysed. Using glacial acetic acid as a catalyst, 5-(pyridin-4-yl)-4H-1,2,4-triazole-3-thiol was condensed with a variety of substituted benzaldehydes in ethanol to yield the target compounds. IR, ¹H NMR, ¹³C NMR, and mass spectrometry were used to confirm the chemical structures of the resulting derivatives. Numerous compounds showed promising multi-targeted biological profiles, according to biological evaluation. With the strongest anticancer activity and a low IC50 value, compound 7f showed great cytotoxic efficacy. In the albumin denaturation test, compound 7b demonstrated the highest percentage inhibition and outstanding anti-inflammatory activity. Furthermore, antimicrobial investigations revealed that 7e had remarkable antifungal activity against Candida albicans, whereas 7b shown notable zones of inhibition against Escherichia coli and Staphylococcus aureus. The results suggest that the biological activity profile is significantly impacted by the addition of various substituents to the benzylidene molecule. The study indicates that the 1,2,4-triazole-3-thiol scaffold is a potential basic component for the creation of multipurpose medicinal drugs with strong anti-inflammatory, anti-microbial, and anti-cancer effects.

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Publication Details

Journal
Zenodo (CERN European Organization for Nuclear Research)
Published
2026-05-01
DOI
https://doi.org/10.5281/zenodo.19909984
Primary Topic
Synthesis and biological activity
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article
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article

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 4-((SUBSTITUTED BENZYLIDENE)AMINO)-5-(PYRIDIN-4-YL)-4H-1,2,4-TRIAZOLE-3-THIOL DERIVATIVES AS POTENTIAL ANTICANCER, ANTIMICROBIAL AND ANTI-INFLAMMATORY AGENTS

Nileshkumar B. Patel1, Faiyazalam M. Shaikh1*, Vatsal M. Patel1, Mohammed Zuber D. Mulla1, Navin B. Patel2, Piyushkumar D. Patel3
Zenodo (CERN European Organization for Nuclear Research)
Synthesis and biological activity
article

SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF 4-((SUBSTITUTED BENZYLIDENE)AMINO)-5-(PYRIDIN-4-YL)-4H-1,2,4-TRIAZOLE-3-THIOL DERIVATIVES AS POTENTIAL ANTICANCER, ANTIMICROBIAL AND ANTI-INFLAMMATORY AGENTS

Nileshkumar B. Patel1, Faiyazalam M. Shaikh1*, Vatsal M. Patel1, Mohammed Zuber D. Mulla1, Navin B. Patel2, Piyushkumar D. Patel3
article en

Abstract

The anticancer, antimicrobial and anti-inflammatory properties of a novel series of 4-((substituted benzylidene)amino)-5-(pyridin-4-yl)-4H-1,2,4-triazole-3-thiol derivatives were synthesized and analysed. Using glacial acetic acid as a catalyst, 5-(pyridin-4-yl)-4H-1,2,4-triazole-3-thiol was condensed with a variety of substituted benzaldehydes in ethanol to yield the target compounds. IR, ¹H NMR, ¹³C NMR, and mass spectrometry were used to confirm the chemical structures of the resulting derivatives. Numerous compounds showed promising multi-targeted biological profiles, according to biological evaluation. With the strongest anticancer activity and a low IC50 value, compound 7f showed great cytotoxic efficacy. In the albumin denaturation test, compound 7b demonstrated the highest percentage inhibition and outstanding anti-inflammatory activity. Furthermore, antimicrobial investigations revealed that 7e had remarkable antifungal activity against Candida albicans, whereas 7b shown notable zones of inhibition against Escherichia coli and Staphylococcus aureus. The results suggest that the biological activity profile is significantly impacted by the addition of various substituents to the benzylidene molecule. The study indicates that the 1,2,4-triazole-3-thiol scaffold is a potential basic component for the creation of multipurpose medicinal drugs with strong anti-inflammatory, anti-microbial, and anti-cancer effects.

Zenodo (CERN European Organization for Nuclear Research)
Openalex Percentile: Top 8%
Synthesis and biological activity
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