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Novel pyridyl nitrofuranyl isoxazolines show antibacterial activity against multiple drug resistant Staphylococcus species.
Picconi, Pietro; Prabaharan, Priya; Auer, Jennifer L; Sandiford, Stephanie; Cascio, Francesco; Chowdhury, Madiha; Hind, Charlotte; Wand, Matthew E; Sutton, J Mark; Rahman, Khondaker M.
Afiliación
  • Picconi P; Institute of Pharmaceutical Science, King's College London, London SE1 1DB, UK.
  • Prabaharan P; Institute of Pharmaceutical Science, King's College London, London SE1 1DB, UK.
  • Auer JL; Institute of Pharmaceutical Science, King's College London, London SE1 1DB, UK.
  • Sandiford S; Public Health England, National Infections Service, Porton Down, Salisbury SP4 0JG, Wiltshire, UK.
  • Cascio F; Institute of Pharmaceutical Science, King's College London, London SE1 1DB, UK.
  • Chowdhury M; Institute of Pharmaceutical Science, King's College London, London SE1 1DB, UK.
  • Hind C; Public Health England, National Infections Service, Porton Down, Salisbury SP4 0JG, Wiltshire, UK.
  • Wand ME; Public Health England, National Infections Service, Porton Down, Salisbury SP4 0JG, Wiltshire, UK.
  • Sutton JM; Public Health England, National Infections Service, Porton Down, Salisbury SP4 0JG, Wiltshire, UK. Electronic address: mark.sutton@phe.gov.uk.
  • Rahman KM; Institute of Pharmaceutical Science, King's College London, London SE1 1DB, UK. Electronic address: k.miraz.rahman@kcl.ac.uk.
Bioorg Med Chem ; 25(15): 3971-3979, 2017 08 01.
Article en En | MEDLINE | ID: mdl-28600080
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oxazoles / Staphylococcus aureus / Farmacorresistencia Bacteriana Múltiple / Antibacterianos / Nitrofurantoína Límite: Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Oxazoles / Staphylococcus aureus / Farmacorresistencia Bacteriana Múltiple / Antibacterianos / Nitrofurantoína Límite: Humans Idioma: En Revista: Bioorg Med Chem Asunto de la revista: BIOQUIMICA / QUIMICA Año: 2017 Tipo del documento: Article Pais de publicación: Reino Unido