Details

Autor(en) / Beteiligte

• Wiener, John J.M.
• Wickboldt, Alvah Tyson
• Nguyen, Steven
• Sun, Siquan
• Rynberg, Raymond
• Rizzolio, Michele
• Karlsson, Lars
• Edwards, James P.
• Grice, Cheryl A.

Titel

Pyrazole-based arylalkyne Cathepsin S inhibitors. Part III: Modification of P4 region

Ist Teil von

• Bioorganic & medicinal chemistry letters, 2013-02, Vol.23 (4), p.1070-1074

Ort / Verlag

England: Elsevier Ltd

Erscheinungsjahr

2013

Quelle

Access via ScienceDirect (Elsevier)

Beschreibungen/Notizen

• Novel classes of tetrahydropyrido-pyrazole thioether amines and arylalkynes that display potency against human Cathepsin S have been previously reported. Here, key pharmacophoric elements of these two classes are merged, and SAR investigations of the P4 region are described, in conjunction with re-optimization of the P5 and P1/P1′/P3 regions. Identification of meta-substituted arylalkynes with good potency and improved solubility is described.