RESUMO
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.
Assuntos
Amidinas/síntese química , Amidinas/farmacologia , Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Candida albicans/efeitos dos fármacos , Bactérias Gram-Negativas/efeitos dos fármacos , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Humanos , Teste de Materiais , Testes de Sensibilidade Microbiana , Reprodutibilidade dos Testes , Espectrofotometria Infravermelho , Sais de Tetrazólio , Tiazóis , Testes de ToxicidadeRESUMO
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.
Assuntos
Humanos , Candida albicans/efeitos dos fármacos , Amidinas/síntese química , Amidinas/farmacologia , Bactérias Gram-Negativas/efeitos dos fármacos , Anti-Infecciosos/síntese química , Anti-Infecciosos/farmacologia , Espectrofotometria Infravermelho , Sais de Tetrazólio , Tiazóis , Teste de Materiais , Testes de Sensibilidade Microbiana , Reprodutibilidade dos Testes , Testes de Toxicidade , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacosRESUMO
A simple, rapid, and sensitive method for the analysis of paroxetine, in tablets as well as the pure drug, by circular dichroism is described. The method was validated for repeatability, linearity, limit of detection, limit of quantification, and recovery according to the International Conference on Harmonization guidelines. Excellent results were obtained, within the globally accepted validation reference values, particularly taking into account the low concentration levels investigated. This is the first report of the quantitation of paroxetine, a chiral drug, without previous separation of the analyte. Additionally, the solid state CD spectrum of PXT was obtained.
