Arylaminoethyl amides as novel non-covalent cathepsin K inhibitors

被引：45

作者：

Altmann, E ^{[1
]}

Renaud, J

Green, J

Farley, D

Cutting, B

Jahnke, W

机构：

[1] Novartis Pharma Res, Arthrit & Bone Metab Therapeut Area, CH-4002 Basel, Switzerland

[2] Novartis Pharma Res, Cent Technol, CH-4002 Basel, Switzerland

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2002年 / 45卷 / 12期

关键词：

D O I：

10.1021/jm010801s

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 (IC50 < 0.006 muM) and are characterized by an excellent selectivity profile vs human cathepsins L and S.

引用

页码：2352 / 2354

页数：3

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