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

Pietro Picconi, Priya Prabaharan, Jennifer L. Auer, Stephanie Sandiford, Francesco Cascio, Madiha Chowdhury, Charlotte Hind, Matthew Wand, J. Mark Sutton, Khondaker M. Rahman

Research output: Contribution to journalArticlepeer-review

7 Citations (Scopus)

Abstract

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 of Staphylococcus strains compared to nitrofuran group containing antibiotic nitrofurantoin.

Original languageEnglish
Pages (from-to)3971-3979
Number of pages9
JournalBioorganic and Medicinal Chemistry
Volume25
Issue number15
DOIs
Publication statusPublished - 2017

Keywords

  • Antibacterial activity
  • Antimicrobial resistance
  • Medicinal chemistry
  • MRSA
  • Nitrofuran isoxazoline
  • Structure activity relationship

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