913180-82-2Relevant academic research and scientific papers
Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: Heterocyclic P3
Tully, David C.,Liu, Hong,Alper, Phil B.,Chatterjee, Arnab K.,Epple, Robert,Roberts, Michael J.,Williams, Jennifer A.,Nguyen, Khanhlinh T.,Woodmansee, David H.,Tumanut, Christine,Li, Jun,Spraggon, Glen,Chang, Jonathan,Tuntland, Tove,Harris, Jennifer L.,Karanewsky, Donald S.
, p. 1975 - 1980 (2007/10/03)
A series of Nα-2-benzoxazolyl-α-amino acid-(arylaminoethyl)amides were identified as potent, selective, and noncovalent inhibitors of cathepsin S. Structure-activity relationships including strategies for modulating the selectivities among cathepsins S, K, and L, and in vivo pharmacokinetics are discussed. A X-ray structure of compound 3 bound to the active site of cathepsin S is also reported.
Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: 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.
, p. 5112 - 5117 (2007/10/03)
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
