Author/Authors :
Cheryl A. Grice، نويسنده , , Kevin Tays، نويسنده , , Haripada Khatuya، نويسنده , , Darin J. Gustin، نويسنده , , Christopher R. Butler، نويسنده , , Jianmei Wei، نويسنده , , Clark A. Sehon، نويسنده , , Siquan Sun، نويسنده , , Yin Gu، نويسنده , , Wen Jiang، نويسنده , , Robin L. Thurmond، نويسنده , , Lars Karlsson، نويسنده , , James P. Edwards، نويسنده ,
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.
