Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1373002 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
John J.M. Wiener, Alvah Tyson Wickboldt, Steven Nguyen, Siquan Sun, Raymond Rynberg, Michele Rizzolio, Lars Karlsson, James P. Edwards, Cheryl A. Grice,