Benjamin Perez Urzua

Graphical Abstract New macrocyclic plasmin inhibitors containing a C-terminal P1 benzylamine group were synthesized. Their N-terminal substitution provided analogues with sub-nanomolar Ki values. Additional inhibitors containing an asymmetric linker possess Ki values close to 2 nM. For the first time, crystal structures of these macrocyclic inhibitors in complex with a Ser195Ala microplasmin mutant were determined, which explain their excellent potency and selectivity.