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Synthesis, in vitro cytotoxicity, and antibacterial studies of new asymmetric bis-1,2,4-triazoles


A series of asymmetric bis-1,2,4-triazoles (4al) were synthesized from respective 1,2,4-triazole-3-thiocarbohydrazides (2a, b) via base catalyzed dehydrative cyclization of thiosemicarbazide intermediates (3al). The synthesized compounds were characterized by IR, 1H-NMR, 13C-NMR, and Mass spectral studies. The asymmetric bis-1,2,4-triazole derivatives (4al) were evaluated for in vitro antioxidant activity by DPPH radical scavenging assay method. The compounds with significant antioxidant potential were evaluated for in vitro cytotoxicity by MTT assay method against HT29 (Human adenocarcinoma) and MDA-231 (Human breast cancer) cancer cell lines. All the synthesized compounds were evaluated for in vitro antibacterial activity against Bacillus subtilus (ATCC 6633), Staphylococcus aureus (ATCC-25923), Escherichia coli (ATCC-25922), and Pseudomonas aeruginosa (ATCC-27853).

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Authors are thankful to The Principal, JSS College of Pharmacy, Mysore, India for providing necessary facilities. Authors express thanks to The Director, NMR research centre, Indian Institute of Science, Bangalore for spectral data.

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Correspondence to Gurubasavaraj V. Pujar.

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Singh, R., Pujar, G.V., Purohit, M.N. et al. Synthesis, in vitro cytotoxicity, and antibacterial studies of new asymmetric bis-1,2,4-triazoles. Med Chem Res 22, 2163–2173 (2013).

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  • Asymmetric bis-1,2,4-triazoles
  • DPPH radical scavenging
  • MTT assay