Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities
AUTOR(ES)
MONTE, ZENAIDE S., SILVA, AMANDA M., LIMA, GLÁUCIA M.S., SILVA, TERESINHA G. DA, MARQUES, KARLA M.R., RODRIGUES, MARIA D., FALCÃO, EMERSON P.S., MELO, SEBASTIÃO J.
FONTE
An. Acad. Bras. Ciênc.
DATA DE PUBLICAÇÃO
2017-06
RESUMO
ABSTRACT 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.
Documentos Relacionados
- Evaluation of antimicrobial, cytotoxic and chemopreventive activities of carvone and its derivatives
- Synthesis of New trans-Dehydrocrotonin Nitrogenated Derivatives and their Cytotoxic and DNA-Topoisomerase I Inhibitory Activities
- Synthesis and antimicrobial evaluation of some new pyrazole, pyrazoline and chromeno[3,4-c]pyrazole derivatives
- Synthesis of novel kavain-like derivatives and evaluation of their cytotoxic activity
- Synthesis, antimicrobial and cytotoxic activities of 5-benzylidene-2-[(pyridine-4-ylmethylene)hydrazono]-thiazolidin-4-one and 2-[(pyridine-4-ylmethylene) hydrazono]-thiazolidin-4-one derivatives