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Synthesis and Biological Activity of 3-(substitutedphenyl)-6-(4-methoxy phenyl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine: Part II


Niranjan Kaushik*, Nitin Kumar, Anoop Kumar and Vikas Sharma   Pages 1 - 7 ( 7 )


Background: Fungal infections are opportunistic infections that become a serious problem to human health.

Objective: Considering the antifungal potential of triazole nucleus, the study was carried out with the objective to synthesize some novel triazole derivatives with antifungal potential.

Method: 1,2,4-triazole derivatives were synthesized via a two step reaction (reported earlier). The first step involves reaction of substituted benzoic acid with thiocarbohydrazide to form 4-amino-3-(substituted phenyl)-5-mercapto-1, 2, 4-triazole derivatives (1a-1k) while in second step, synthesized compounds (1a-1k) were then subsequently treated with substituted acetophenone to yield substituted (4-methoxyphenyl-7H-[1, 2, 4] triazolo [3, 4-b][1,3,4] thiadiazine derivatives (2a-2k). All synthesized compounds were characterized by IR, 1H NMR, and Mass spectral data analysis and were screened for their antifungal properties against different fungal strains i.e. Candida tropicalis (ATCC-13803, ATCC-20913), Candida albicans (ATCC-60193), Candida inconspicua (ATCC-16783) and Candida glabrata (ATCC-90030, ATCC-2001).

Results: Compound 2d displayed better percentage inhibition (26.29%, 24.81%) than fluconazole (24.44%, 22.96%) against ATCC-16783, ATCC-2001 fungal strains respectively at 100µg/ml. Compound 2f also displayed better percentage inhibition (28.51%) against ATCC-90030 as compared to fluconazone (27.4%) at 200 µg/ml. Similarly, compounds 2e and 2j also exhibited better antifungal properties than fluconazole at 200µg/ml. Compound 2e was found most potent against ATCC13803 (30.37%) and ATCC-90030 (30.37%) fungal strains as compared to fluconazole (28.14%, 27.4%) at 200 µg/ml respectively whereas compound 2j exhibited better antifungal activity (28.51%) against ATCC-60193 than fluconazole (27.7%) at 200 µg/ml.

Conclusion: The results were in accordance with our assertions for triazole derivatives, as all compounds displayed moderate to good antifungal activity.


Triazole, thiadiazine, fluconazole, thiocarbohydrazide, benzoic acid, antifungal activity.


Department of Pharmacy, School of Medical and Allied Sciences, Galgotias University, Greater Noida, Gautam Budh Nagar – 201306, Uttar Pradesh, School of Medical & Allied Sciences, K R Mangalam University, Gurugram, Haryana-122103, Department of Pharmaceutical Technology, Meerut Institute of Engineering & Technology, Meerut – 250005, Uttar Pradesh, IIMT College of Pharmacy, Greater Noida, Uttar Pradesh-201308

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