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Exploration of the P 1 SAR of aldehyde cathepsin K inhibitors

…, AM Hassell, RB McFadyen, AB Miller, LR Miller…

文献索引:Catalano, John G; Deaton, David N; Furfine, Eric S; Hassell, Annie M; McFadyen, Robert B; Miller, Aaron B; Miller, Larry R; Shewchuk, Lisa M; Willard Jr., Derril H; Wright, Lois L Bioorganic and medicinal chemistry letters, 2004 , vol. 14, # 1 p. 275 - 278

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被引用次数: 41

摘要

The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S1 subsite with a series of α-amino aldehyde derivatives substituted at the P1 position afforded compounds with cathepsin K IC50s between 52 μM and 15 nM.