- Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus
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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.
- Kyei-Baffour, Kwaku,Mohammad, Haroon,Seleem, Mohamed N.,Dai, Mingji
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p. 1845 - 1854
(2019/03/28)
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- Studies on antiulcer drugs. V. Synthesis and antiulcer activity of aralkylbenzazoles
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A series of 2-alkylamino-5- or 6-aralkyl-substituted benzazoles were synthesized and tested for histamine H2-receptor antagonist and anti-stress ulcer activities. These new compounds showed little or no histamine H2-receptor antagoni
- Katsura,Inoue,Tomoi,Takasugi
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p. 2062 - 2074
(2007/10/02)
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