Document Report Card

ID: ALA1135429

Journal: J Med Chem

Title: Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors.

Authors: Altmann E, Renaud J, Green J, Farley D, Cutting B, Jahnke W.

Abstract: A series of N(alpha)-benzyloxycarbonyl- and N(alpha)-acyl-L-leucine(2-phenylaminoethyl)amide derivatives were prepared and evaluated for their inhibitory activity against rabbit and human cysteine proteases cathepsins K, L, and S. These data indicate that N(alpha)-acyl-alpha-amino acid-(arylaminoethyl)amides represent a new class of selective non-covalent inhibitors of cathepsin K. Compounds 4b, 4e, and 4g exhibit high potency toward rabbit and human cathepsin K (IC(50) < 0.006 microM) and are characterized by an excellent selectivity profile vs human cathepsins L and S.

CiteXplore: 12036343

DOI: 10.1021/jm010801s