1227072-07-2Relevant academic research and scientific papers
Discovery and SAR of novel pyrazole-based thioethers as cathepsin S inhibitors. Part 2: Modification of P3, P4, and P5 regions
Wiener, John J.M.,Wickboldt Jr., Alvah T.,Wiener, Danielle K.,Lee-Dutra, Alice,Edwards, James P.,Karlsson, Lars,Nguyen, Steven,Sun, Siquan,Jones, Todd K.,Grice, Cheryl A.
, p. 2375 - 2378 (2010)
A novel class of tetrahydropyrido-pyrazole thioether amines that display potency against human Cathepsin S have been previously reported. Here, further SAR investigations of the P3, P4, and P5 regions are described. In particular, 4-fluoropiperidine is identified as a competent P3 binding element when utilized in conjunction with a (S)-2-hydroxypropyl linker-containing P5 moiety and oxamide or sulfonamide P4 substitution.
