762289-11-2Relevant articles and documents
Novel broad-spectrum inhibitors of bacterial methionine aminopeptidase
Rose, Jonathan A.,Lahiri, Sushmita D.,McKinney, David C.,Albert, Rob,Morningstar, Marshall L.,Shapiro, Adam B.,Fisher, Stewart L.,Fleming, Paul R.
, p. 3301 - 3306 (2015)
With increasing emergence of multi-drug resistant infections, there is a dire need for new classes of compounds that act through unique mechanisms. In this work, we describe the discovery and optimization of a novel series of inhibitors of bacterial methionine aminopeptidase (MAP). Through a high-throughput screening campaign, one azepinone amide hit was found that resembled the native peptide substrate and possessed moderate biochemical potency against three bacterial isozymes. X-ray crystallography was used in combination with substrate-based design to direct the rational optimization of analogs with sub-micromolar potency. The novel compounds presented here represent potent broad-spectrum biochemical inhibitors of bacterial MAP and have the potential to lead to the development of new medicines to combat serious multi-drug resistant infections.
NOVEL LACTAMS AND USES THEREOF
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Page 42; 44, (2010/02/08)
This invention relates to novel compounds having formula (I) to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit secretase and thereby inhibit the production of amyloid ? protein, thereby acting to prevent the formation of neurological deposits of amyloid protein. The present invention relates to the treatment of neurological disorders related to amyloid ? - protein production such as Alzheimer's disease.
