Design and synthesis of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 1 |
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| Authors: | Liu Hong Tully David C Epple Robert Bursulaya Badry Li Jun Harris Jennifer L Williams Jennifer A Russo Ross Tumanut Christine Roberts Michael J Alper Phil B He Yun Karanewsky Donald S |
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| Institution: | Genomics Institute of the Novartis Research Foundation, 10675 John J. Hopkins Dr., San Diego, CA 92121, USA. hliu@gnf.org |
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| Abstract: | A series of Nalpha-acyl-alpha-amino acid-(arylaminoethyl)amides were found to be potent and noncovalent cathepsin S inhibitors. Compound 20 possessed high cathepsin S affinity (Ki=3.3 nM) and showed excellent selectivity over cathepsin K, L, F, and V. Molecular modeling, design, synthesis, and in vitro activity are described. |
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