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ID: ALA1147461

Journal: Bioorg Med Chem Lett

Title: Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors.

Authors: Boros EE, Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Paulick MG, Shewchuk LM, Thompson JB, Willard DH, Wright LL.

Abstract: The synthesis and biological activity of a series of aldehyde inhibitors of cathepsin K are reported. Exploration of the properties of the S2 and S3 subsites with a series of carbamate derivatized norleucine aldehydes substituted at the P2 and P3 positions afforded analogs with cathepsin K IC50s between 600 nM and 130 pM.

CiteXplore: 15177446

DOI: 10.1016/j.bmcl.2004.04.084