Abstract
A series of novel 1,2,3-thiadiazolo-5-carboxylic acid hydrazide Schiff’s bases 4a–4r were prepared starting from ethyl-4,4,4-trifluoroacetoacetate and ethyl carbazate in four steps. All the compounds were screened for antibacterial activity against various bacterial strains at 150 μg/ml concentration and found no activity. Similarly, all the compounds were screened for antifungal activity against various fungal strains at 100 and 150 μg/ml concentrations. Compounds 4a, 4m, and 4q found to show moderate activity against Candida albicans. Further, compounds were evaluated for cytotoxic activity against breast carcinoma cells MDA-MB 231 (aggressive), MCF-7 (non-aggressive) using doxorubicin as standard. Compound 4n was found to show 25.39 % cell viability against MDA-MB 231 and 63.60 % cell viability against MCF-7 cells.
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Acknowledgments
Authors are thankful to Dr. J.S.Yadav, Director, IICT for his constant encouragement and authors (P. Sambasiva Rao, C. Kurumurthy, B. Veeraswamy, and G. Santhosh kumar) are thankful to CSIR for providing financial assistance in the form of Senior Research Fellowship.
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Sambasiva Rao, P., Kurumurthy, C., Veeraswamy, B. et al. Synthesis, antimicrobial and cytotoxic activities of novel 4-trifluoromethyl-(1,2,3)-thiadiazolo-5-carboxylic acid hydrazide Schiff’s bases. Med Chem Res 22, 1747–1755 (2013). https://doi.org/10.1007/s00044-012-0168-x
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DOI: https://doi.org/10.1007/s00044-012-0168-x