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Bioorg Med Chem ; 25(15): 3971-3979, 2017 08 01.
Artículo en Inglés | MEDLINE | ID: mdl-28600080

RESUMEN

A novel series of pyridyl nitrofuranyl isoxazolines were synthesized and evaluated for their antibacterial activity against multiple drug resistant (MDR) Staphylococcus strains. Compounds with piperazine linker between the pyridyl group and isoxazoline ring showed better activity when compared to compounds without the piperazine linker. 3-Pyridyl nitrofuranyl isoxazoline with a piperazine linker was found to be more active than corresponding 2-and 4-pyridyl analogues with MICs in the range of 4-32µg/mL against MDR Staphylococcus strains. The eukaryotic toxicity of the compounds was tested by MTT assay and were found to be non-toxic against both non-tumour lung fibroblast WI-38 and cervical cancer cell line HeLa. The most active pyridyl nitrofuranyl isoxazoline compound showed improved activity against a panel of Staphylococcus strains compared to nitrofuran group containing antibiotic nitrofurantoin.


Asunto(s)
Antibacterianos/farmacología , Farmacorresistencia Bacteriana Múltiple/efectos de los fármacos , Nitrofurantoína/química , Oxazoles/farmacología , Staphylococcus aureus/efectos de los fármacos , Antibacterianos/química , Línea Celular Tumoral , Humanos , Pruebas de Sensibilidad Microbiana , Oxazoles/química , Análisis Espectral , Relación Estructura-Actividad
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