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 L.
AU - Sandiford, Stephanie
AU - Cascio, Francesco
AU - Chowdhury, Madiha
AU - Hind, Charlotte
AU - Wand, Matthew
AU - Sutton, J. Mark
AU - Rahman, Khondaker M.
N1 - Publisher Copyright:
© 2017 Elsevier Ltd
Copyright:
Copyright 2017 Elsevier B.V., All rights reserved.
PY - 2017
Y1 - 2017
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 of 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 of Staphylococcus strains compared to nitrofuran group containing antibiotic nitrofurantoin.
KW - Antibacterial activity
KW - Antimicrobial resistance
KW - Medicinal chemistry
KW - MRSA
KW - Nitrofuran isoxazoline
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
C2 - 28600080
AN - SCOPUS:85020199991
VL - 25
SP - 3971
EP - 3979
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
SN - 0968-0896
IS - 15
ER -
