Thioether acetamides as P3 binding elements for tetrahydropyrido-pyrazole cathepsin S inhibitors |
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| Authors: | Danielle K Wiener Alice Lee-Dutra Scott Bembenek Steven Nguyen Robin L Thurmond Siquan Sun Lars Karlsson Cheryl A Grice Todd K Jones James P Edwards |
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| Institution: | Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, United States |
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| Abstract: | A series of tetrahydropyrido-pyrazole cathepsin S (CatS) inhibitors with thioether acetamide functional groups were prepared with the goal of improving upon the cellular activity of amidoethylthioethers. This Letter describes altered amide connectivity, in conjunction with changes to other binding elements, resulting in improved potency, as well as increased knowledge of the relationship between this chemotype and human CatS activity. |
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