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J Med Chem. 2002 Jun 6;45(12):2352-4.

Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors.

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.

PMID:
12036343
DOI:
10.1021/jm010801s
[Indexed for MEDLINE]

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