King's College London

Research portal

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

Research output: Contribution to journalArticle

Standard

Novel pyridyl nitrofuranyl isoxazolines show antibacterial activity against multiple drug resistant Staphylococcus species. / Picconi, Pietro; Prabaharan, Priya; Auer, Jennifer; Sandiford, Stephanie; Cascio, Francesco; Chowdhury, Madiha; Hind, Charlotte; Wand, Matthew E.; Sutton, J. Mark; Rahman, Khondaker M.

In: Bioorganic and Medicinal Chemistry, 19.05.2017.

Research output: Contribution to journalArticle

Harvard

Picconi, P, Prabaharan, P, Auer, J, Sandiford, S, Cascio, F, Chowdhury, M, Hind, C, Wand, ME, Sutton, JM & Rahman, KM 2017, 'Novel pyridyl nitrofuranyl isoxazolines show antibacterial activity against multiple drug resistant Staphylococcus species.', Bioorganic and Medicinal Chemistry. https://doi.org/10.1016/j.bmc.2017.05.037

APA

Picconi, P., Prabaharan, P., Auer, J., Sandiford, S., Cascio, F., Chowdhury, M., Hind, C., Wand, M. E., Sutton, J. M., & Rahman, K. M. (2017). Novel pyridyl nitrofuranyl isoxazolines show antibacterial activity against multiple drug resistant Staphylococcus species. Bioorganic and Medicinal Chemistry. https://doi.org/10.1016/j.bmc.2017.05.037

Vancouver

Picconi P, Prabaharan P, Auer J, Sandiford S, Cascio F, Chowdhury M et al. Novel pyridyl nitrofuranyl isoxazolines show antibacterial activity against multiple drug resistant Staphylococcus species. Bioorganic and Medicinal Chemistry. 2017 May 19. https://doi.org/10.1016/j.bmc.2017.05.037

Author

Picconi, Pietro ; Prabaharan, Priya ; Auer, Jennifer ; Sandiford, Stephanie ; Cascio, Francesco ; Chowdhury, Madiha ; Hind, Charlotte ; Wand, Matthew E. ; Sutton, J. Mark ; Rahman, Khondaker M. / Novel pyridyl nitrofuranyl isoxazolines show antibacterial activity against multiple drug resistant Staphylococcus species. In: Bioorganic and Medicinal Chemistry. 2017.

Bibtex Download

@article{88b0c29cbc03426dbd87daeace7c75ab,
title = "Novel pyridyl nitrofuranyl isoxazolines show antibacterial activity against multiple drug resistant Staphylococcus species.",
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 Staphylococcus strains compared to nitrofuran group containing antibiotic nitrofurantoin.",
keywords = "Antimicrobial Resistance, Nitrofuran Isoxazoline, MRSA, Medicinal Chemistry, Antibacterial Activity, Structure Activity Relationship",
author = "Pietro Picconi and Priya Prabaharan and Jennifer Auer and Stephanie Sandiford and Francesco Cascio and Madiha Chowdhury and Charlotte Hind and Wand, {Matthew E.} and Sutton, {J. Mark} and Rahman, {Khondaker M.}",
year = "2017",
month = may,
day = "19",
doi = "10.1016/j.bmc.2017.05.037",
language = "English",
journal = "Bioorganic and Medicinal Chemistry",
issn = "0968-0896",
publisher = "Elsevier Limited",

}

RIS (suitable for import to EndNote) Download

TY - JOUR

T1 - Novel pyridyl nitrofuranyl isoxazolines show antibacterial activity against multiple drug resistant Staphylococcus species.

AU - Picconi, Pietro

AU - Prabaharan, Priya

AU - Auer, Jennifer

AU - Sandiford, Stephanie

AU - Cascio, Francesco

AU - Chowdhury, Madiha

AU - Hind, Charlotte

AU - Wand, Matthew E.

AU - Sutton, J. Mark

AU - Rahman, Khondaker M.

PY - 2017/5/19

Y1 - 2017/5/19

N2 - 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.

AB - 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.

KW - Antimicrobial Resistance

KW - Nitrofuran Isoxazoline

KW - MRSA

KW - Medicinal Chemistry

KW - Antibacterial Activity

KW - Structure Activity Relationship

UR - http://www.scopus.com/inward/record.url?scp=85020199991&partnerID=8YFLogxK

U2 - 10.1016/j.bmc.2017.05.037

DO - 10.1016/j.bmc.2017.05.037

M3 - Article

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

SN - 0968-0896

ER -

View graph of relations

© 2018 King's College London | Strand | London WC2R 2LS | England | United Kingdom | Tel +44 (0)20 7836 5454