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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 4-32µg/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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Picconi P,Prabaharan P,Auer JL,Sandiford S,Cascio F,Chowdhury M,Hind C,Wand ME,Sutton JM,Rahman KM

doi

10.1016/j.bmc.2017.05.037

subject

Has Abstract

pub_date

2017-08-01 00:00:00

pages

3971-3979

issue

15

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(17)30690-9

journal_volume

25

pub_type

杂志文章

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