A series of arylamidines 3a-j was designed, synthesized and investigated for antimicrobial activity. Structures of the compounds were confirmed by IR, 1H-NMR and 13C-NMR and a 2D spectroscopic study was performed. A preliminary screening of the antimicrobial tests clearly showed that three out of ten arylamidines, viz, 3f, 3g and 3i, were effective against all the gram-negative bacteria: Klebsiella pneumoniae, Pseudomonas aeruginosa and Salmonella enteric; and against the yeast, candida albicans. Further, the Minimum Inhibitory Concentrations (MIC) against the bacteria and yeast were determined. All compounds 3a-d, 3f, 3g, 3i and 3j were also investigated for their low cytotoxic effects on tested cell lines. Compounds 3d and 3f were the most effective derivatives against HL-60 and HEp-2 cells, respectively, with IC50 value (2μg/mL), and low normal cells toxicity.
CITATION STYLE
Monte, Z. S., Silva, A. M., Lima, G. M. S., Da Silva, T. G., Marques, K. M. R., Rodrigues, M. D., … de Melo, S. J. (2017). Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities. Anais Da Academia Brasileira de Ciencias, 89(2), 1051–1058. https://doi.org/10.1590/0001-3765201720160801
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