Synthesis and SAR of succinamide peptidomimetic inhibitors of cathepsin S

…, J Chang, P Gordon, T Hollenbeck, C Tumanut…

文献索引：Chatterjee, Arnab K.; Liu, Hong; Tully, David C.; Guo, Jianhua; Epple, Robert; Russo, Ross; Williams, Jennifer; Roberts, Michael; Tuntland, Tove; Chang, Jonathan; Gordon, Perry; Hollenbeck, Thomas; Tumanut, Christine; Li, Jun; Harris, Jennifer L. Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 10 p. 2899 - 2903

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被引用次数: 21

摘要

Peptidic, non-covalent inhibitors of lysosomal cysteine protease cathepsin S (1 and 2) were investigated due to low oral bioavailability, leading to an improved series of peptidomimetic inhibitors. Utilizing phenyl succinamides as the P2 residue increased the oral exposure of this lead series of compounds, while retaining selective inhibition of the cathepsin S isoform. Concurrent investigation of the P1 and P2 subsites resulted in the discovery of several ...