A novel amino-benzosuberone derivative is a picomolar inhibitor of mammalian aminopeptidase N/CD13.

@article{Maiereanu2011ANA,
  title={A novel amino-benzosuberone derivative is a picomolar inhibitor of mammalian aminopeptidase N/CD13.},
  author={Carmen Maiereanu and C{\'e}line Schmitt and Nad{\`e}ge Schifano-Faux and Didier Le Nou{\"e}n and Albert Defoin and C{\'e}line Tarnus},
  journal={Bioorganic & medicinal chemistry},
  year={2011},
  volume={19 18},
  pages={5716-33}
}
A new class of low molecular weight, highly potent and selective non peptidic inhibitors of aminopeptidase N (APN/CD13) is described. We report the synthesis and in vitro evaluation of racemic substituted analogues of 7-amino-benzocyclohepten-6-one 1a. We investigated various substitutions on the aromatic ring with phenyl and halogen groups. In vitro kinetic studies revealed that these compounds are among the most effective APN/CD13 inhibitors found so far. Hydrophobic substituents placed at… CONTINUE READING