Novel pyridyl nitrofuranyl isoxazolines show antibacterial activity against multiple drug resistant Staphylococcus species.

Publication date: Available online 19 May 2017
Source:Bioorganic & Medicinal Chemistry
Author(s): Pietro Picconi, Priya Prabaharan, Jennifer Auer, Stephanie Sandiford, Francesco Cascio, Madiha Chowdhury, Charlotte Hind, Matthew E. Wand, J. Mark Sutton, Khondaker M. Rahman
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 4-32 µg/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 Staphylococcus strains compared to nitrofuran group containing antibiotic nitrofurantoin.

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