5 research outputs found
Focus on the Future: A Plan for the HOPE Village Initiative Area
http://deepblue.lib.umich.edu/bitstream/2027.42/110953/1/focusonthefuture2010.pd
Seven-membered ring scaffolds for drug discovery: access to functionalised azepanes and oxepanes through diazocarbonyl chemistry
Functionalised azepane and oxepane scaffolds were prepared using diazocarbonyl chemistry and elaborated to show their potential use in library synthesis. Key dicarbonyl containing seven-membered rings were functionalised via diastereoselective Luche reduction of the ketone followed by manipulation of the ester and amine groups. Further scaffolds could be accessed by C-alkylation of the dicarbonyl compounds. In addition, an oxepane containing amino acid could be prepared via a diastereoselective enamine reduction
Pyridone Methylsulfone Hydroxamate LpxC Inhibitors for the Treatment of Serious Gram-Negative Infections
The synthesis and biological activity of a new series
of LpxC inhibitors represented by pyridone methylsulfone hydroxamate <b>2a</b> is presented. Members of this series have improved solubility
and free fraction when compared to compounds in the previously described
biphenyl methylsulfone hydroxamate series, and they maintain superior
Gram-negative antibacterial activity to comparator agents