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Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus.

Abstract：

:Antibiotic resistance remains a major global public health threat that requires sustained discovery of novel antibacterial agents with unexploited scaffolds. Structure-activity relationship of the first-generation aryl isonitrile compounds we synthesized led to an initial lead molecule that informed the synthesis of a second-generation of aryl isonitriles. From this new series of 20 compounds, three analogues inhibited growth of methicillin-resistant Staphylococcus aureus (MRSA) (from 1 to 4 µM) and were safe to human keratinocytes. Compound 19, with an additional isonitrile group exhibited improved activity against MRSA compared to the first-generation lead compound. This compound emerged as a candidate worthy of further investigation and further reinforced the importance of the isonitrile functionality in the compounds' anti-MRSA activity. In a murine skin wound model, 19 significantly reduced the burden of MRSA, similar to the antibiotic fusidic acid. In summary, 19 was identified as a new lead aryl isonitrile compound effective against MRSA.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Kyei-Baffour K,Mohammad H,Seleem MN,Dai M

doi

10.1016/j.bmc.2019.03.034

subject

Has Abstract

pub_date

2019-05-01 00:00:00

pages

1845-1854

issue

9

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(19)30262-7

journal_volume

27

pub_type

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