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The SAR of 4-substituted (6,6-bicyclic) piperidine cathepsin S inhibitors.

Abstract：

:A series of competitive, reversible cathepsin S (CatS) inhibitors was investigated. An earlier disclosure detailed the discovery of the 4-(2-keto-1-benzimidazolinyl)-piperidin-1-yl moiety as an effective replacement for the 4-arylpiperazin-1-yl group found in our screening hit. Continued investigation into replacements for the 4-aryl piperazine resulted in the identification of potentially useful CatS inhibitors with enzymatic and cellular activity similar to that of JNJ 10329670 as disclosed in a previous publication.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Grice CA,Tays K,Khatuya H,Gustin DJ,Butler CR,Wei J,Sehon CA,Sun S,Gu Y,Jiang W,Thurmond RL,Karlsson L,Edwards JP

doi

10.1016/j.bmcl.2006.01.038

subject

Has Abstract

pub_date

2006-04-15 00:00:00

pages

2209-12

issue

8

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(06)00075-8

journal_volume

16

pub_type

杂志文章

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