Bioorganic and Medicinal Chemistry Letters p. 5112 - 5117 (2006)
Update date:2022-08-03
Topics: Synthesis Cathepsin S SAR (Structure-Activity Relationship) Arylaminoethyl amides Noncovalent inhibitors P3 cyclic ethers
Tully, David C.
Liu, Hong
Chatterjee, Arnab K.
Alper, Phil B.
Epple, Robert
Williams, Jennifer A.
Roberts, Michael J.
Woodmansee, David H.
Masick, Brian T.
Tumanut, Christine
Li, Jun
Spraggon, Glen
Hornsby, Michael
Chang, Jonathan
Tuntland, Tove
Hollenbeck, Thomas
Gordon, Perry
Harris, Jennifer L.
Karanewsky, Donald S.
The synthesis and structure-activity relationship of a series of arylaminoethyl amide cathepsin S inhibitors are reported. Optimization of P3 and P2 groups to improve overall physicochemical properties resulted in significant improvements in oral bioavail
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