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Exploration of the P1 SAR of aldehyde cathepsin K inhibitors |
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| Authors: | 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 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 S(1) subsite with a series of alpha-amino aldehyde derivatives substituted at the P(1) position afforded compounds with cathepsin K IC(50)s between 52 microM and 15 nM. |
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