Your browser doesn't support javascript.
loading
Mostrar: 20 | 50 | 100
Resultados 1 - 1 de 1
Filtrar
Mais filtros










Base de dados
Intervalo de ano de publicação
1.
PLoS One ; 8(3): e58346, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-23554886

RESUMO

Keratitis treatment has become more complicated due to the emergence of bacterial or fungal pathogens with enhanced antibiotic resistance. The pharmaceutical applications of N-heterocyclic carbene complexes have received remarkable attention due to their antimicrobial properties. In this paper, the new precursor, 3,3'-(p-phenylenedimethylene) bis{1-(2- methyl-allyl)imidazolium} bromide (1a) and its analogous PF6 salt (1b) were synthesized. Furthermore, silver(I) and gold(I) -N-heterocyclic carbene (NHC) complexes [Ag2LBr2/Au2LBr2; 2a/3a], [(Ag2L2)(PF6)2/(Au2L2)(PF6)2; 2b/3b] were developed from their corresponding ligands. All compounds were screened for their antimicrobial activities against multiple keratitis-associated human eye pathogens, including bacteria and fungi. Complexes 2a and 3a showed highest activity, and the effectiveness of 3a was also studied, focusing eradication of pathogen biofilm. Furthermore, the structures of 1a, 2a and 3b were determined using single crystal X-ray analysis, 2b and 3a were optimized theoretically. The mechanism of action of 3a was evaluated by scanning electron microscopy and docking experiments, suggesting that its target is the cell membrane. In summary, 3a may be helpful in developing antimicrobial therapies in patients suffering from keratitis-associated eye infections caused by multidrug-resistant pathogens.


Assuntos
Alcenos/farmacologia , Anti-Infecciosos/farmacologia , Biofilmes , Infecções Oculares/tratamento farmacológico , Ouro/farmacologia , Imidazóis/farmacologia , Ceratite/tratamento farmacológico , Alcenos/síntese química , Alcenos/química , Animais , Anti-Infecciosos/síntese química , Anti-Infecciosos/química , Linhagem Celular Tumoral , Lentes de Contato/microbiologia , Lentes de Contato de Uso Prolongado , Infecções Oculares/etiologia , Infecções Oculares/microbiologia , Ouro/química , Humanos , Imidazóis/química , Ceratite/complicações , Ceratite/microbiologia , Camundongos
SELEÇÃO DE REFERÊNCIAS
DETALHE DA PESQUISA
...