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Exploration of the P2-P3 SAR of aldehyde cathepsin K inhibitors |
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| Authors: | Boros Eric E Deaton David N Hassell Anne M McFadyen Robert B Miller Aaron B Miller Larry R Paulick Margot G Shewchuk Lisa M Thompson James B Willard Derril H Wright Lois L |
| Affiliation: | Department of Medicinal Chemistry, GlaxoSmithKline, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA. |
| 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. |
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