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(4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors |
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| Authors: | Kim Tae-Seong Hague Andrew B Lee Tony I Lian Brian Tegley Christopher M Wang Xianghong Burgess Teresa L Qian Yi-Xin Ross Sandra Tagari Philip Lin Chi-Hwei Mayeda Carol Dao Jennifer Jordan Steven Mohr Christopher Cheetham Janet Viswanadhan Vellarkad Tasker Andrew S |
| Affiliation: | Department of Chemistry Research and Development, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320-1799, USA. tkim@amgen.com |
| Abstract: | A series of (4-piperidinylphenyl)aminoethyl amides based on dipeptide anilines were synthesized and tested against cathepsin K, cathepsin L and cathepsin B. These new non-covalent inhibitors exhibited single-digit nM inhibition of the cysteine proteases. Compounds 3 and 7 demonstrated potency in both mouse and human osteoclast resorption assays. |
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