Author/Authors :
Eva Altmann، نويسنده , , Reiner Aichholz، نويسنده , , Claudia Betschart، نويسنده , , Thomas Buhl، نويسنده , , Jonathan Green، نويسنده , , René Lattmann، نويسنده , , Martin Missbach، نويسنده ,
Abstract :
A series of dipeptidyl nitriles as inhibitors of cathepsin K have been explored starting from lead structure 1 (Cbz–Leu–NH–CH2–CN, IC50 = 39 nM). Attachment of non-natural amino acid side chains in P1 and modification of the P3 subunit led to inhibitors with higher potency and improved pharmacokinetic properties.
