1049809-74-6Relevant articles and documents
Pyrazole-based arylalkyne Cathepsin S inhibitors. Part III: Modification of P4 region
Wiener, John J.M.,Wickboldt, Alvah Tyson,Nguyen, Steven,Sun, Siquan,Rynberg, Raymond,Rizzolio, Michele,Karlsson, Lars,Edwards, James P.,Grice, Cheryl A.
, p. 1070 - 1074 (2013/03/13)
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.