Details

Autor(en) / Beteiligte

• 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

Titel

Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities

Ist Teil von

• Anais da Academia Brasileira de Ciências, 2017-06, Vol.89 (2), p.1051-1059

Ort / Verlag

Brazil: Academia Brasileira de Ciências

Erscheinungsjahr

2017

Quelle

Free E-Journal (出版社公開部分のみ）

Beschreibungen/Notizen

• 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.