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

Some racemic amino-benzosuberones 1a-h′, were synthesised and evaluated as inhibitors of four representative members of zinc-dependent amino-peptidases. Ki values in the nanomolar to picomolar range were obtained selectively against the 'one zinc' aminopeptidase AP-N/CD13. The bromo-phenyl derivative 1d′ belongs to the most potent and selective non-peptidic known inhibitor (Ki = 60 pM).