Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part I

作者：Liu H^*; Tully DC; Epple R; Bursulaya B; Li J; Harris JL; Williams JA; Russo R; Tumanut C; Roberts MJ; Alper PB; He Y; Karanewsky DS

来源：Bioorganic & Medicinal Chemistry Letters, 2005, 15(22): 4979-4984.

DOI：10.1016/j.bmcl.2005.08.017

• cathepsin S
• cathepsin
• cysteine protease inhibitor
• peptidomimetics
• noncovalent inhibitors

A series of N-alpha-acyl-alpha-amino acid-(arylaminoethyl)amides were found to be potent and noncovalent cathepsin S inhibitors. Compound 20 possessed high cathepsin S affinity (K-i = 3.3 nM) and showed excellent selectivity over cathepsin K, L, F, and V. Molecular modeling, design, synthesis, and in vitro activity are described.

• 出版日期2005-11-15