27892-99-5Relevant academic research and scientific papers
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus
Kyei-Baffour, Kwaku,Mohammad, Haroon,Seleem, Mohamed N.,Dai, Mingji
supporting information, p. 1845 - 1854 (2019/03/28)
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.
Heck reactions using segmented flow conditions
Ahmed-Omer, Batoul,Barrow, David A.,Wirth, Thomas
scheme or table, p. 3352 - 3355 (2009/08/17)
Various Heck couplings have been carried out using segmented flow conditions to accelerate the reactions. Aryl iodides and aryl bromides as well as anilines in diazonium-type Heck reactions have been used successfully.
Novel Bis as Antitrypanosomal Agents
Turner, William R.,Werbel, Leslie M.
, p. 1728 - 1740 (2007/10/02)
A series of novel 1,1'-(4,1-phenylene)bis was prepared and evaluated for activity against Trypanosoma rhodesiense in mice.The importance of the bis structure and the nature of the spacer between the two phenyl rings for optimal activity have been revealed.The potent parenteral activity of several analogues within this series as well as preliminary indication of oral activity lends encouragement to further development of this structural class.
