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Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3 |
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| Authors: | Tully David C Liu Hong Alper Phil B Chatterjee Arnab K Epple Robert Roberts Michael J Williams Jennifer A Nguyen KhanhLinh T Woodmansee David H Tumanut Christine Li Jun Spraggon Glen Chang Jonathan Tuntland Tove Harris Jennifer L Karanewsky Donald S |
| Affiliation: | Genomics Institute of the Novartis Research Foundation, 10675 John J. Hopkins Dr., San Diego, CA 92121, USA. dtully@gnf.org |
| Abstract: | A series of N(alpha)-2-benzoxazolyl-alpha-amino acid-(arylaminoethyl)amides were identified as potent, selective, and noncovalent inhibitors of cathepsin S. Structure-activity relationships including strategies for modulating the selectivities among cathepsins S, K, and L, and in vivo pharmacokinetics are discussed. A X-ray structure of compound 3 bound to the active site of cathepsin S is also reported. |
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