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Print version ISSN 0001-3765On-line version ISSN 1678-2690


MONTE, ZENAIDE S. et al. Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities. An. Acad. Bras. Ciênc. [online]. 2017, vol.89, n.2, pp.1051-1059. ISSN 0001-3765.

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.

Keywords : arylamidines; 2D spectroscopy; gram-negative bacteria; yeast; cytotoxicity.

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