Synthesis and biological evaluation of flexible and conformationally constrained LpxC inhibitors.

@article{Lppenberg2013SynthesisAB,
  title={Synthesis and biological evaluation of flexible and conformationally constrained LpxC inhibitors.},
  author={Marius L{\"o}ppenberg and H. M{\"u}ller and Carla Pulina and A. Oddo and M. Teese and J. Jose and Ralph Holl},
  journal={Organic & biomolecular chemistry},
  year={2013},
  volume={11 36},
  pages={
          6056-70
        }
}
Inhibitors of the UDP-3-O-[(R)-3-hydroxymyristoyl]-N-acetylglucosamine deacetylase (LpxC) represent promising candidates for the development of antibiotics possessing a so far unexploited mechanism of action. In a chiral pool synthesis, starting from the D-mannose derived mannonolactone 4, conformationally constrained C-glycosidic as well as open chained hydroxamic acids with a defined stereochemistry were prepared. Diversity was introduced by performing C–C coupling reactions like the… Expand
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