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Bioorg Med Chem Lett. 2006 Apr 15;16(8):2209-12. Epub 2006 Feb 3.

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

Author information

1
Johnson and Johnson Pharmaceutical Research and Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA. cgrice@prdus.jnj.com

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.

PMID:
16458510
DOI:
10.1016/j.bmcl.2006.01.038
[Indexed for MEDLINE]

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