Front Cover: Synthesis and Structural Characterization of Macrocyclic Plasmin Inhibitors (ChemMedChem 6/2023)

The Front Cover shows new macrocyclic plasmin inhibitors containing a C-terminal P1 benzylamine group. Their N-terminal substitution provided analogues with sub-nanomolar Ki values. Additional an asymmetric linker possess values close to 2 nM. For the first time, crystal structures of these in complex Ser195Ala microplasmin mutant were determined, which explain their excellent potency and selectivity. More information can be found Research Article by Simon J. A. Wiedemeyer, Guojie Wu, Ruby H. P. Law, Torsten Steinmetzer et al.