Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: Heterocyclic P3

…, KLT Nguyen, DH Woodmansee, C Tumanut…

文献索引：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. Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 7 p. 1975 - 1980

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被引用次数: 43

摘要

A series of Nα-2-benzoxazolyl-α-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.