119601-26-2Relevant academic research and scientific papers
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
Potent and Selective Inhibitors of an Aspartyl Protease-like Endothelin Converting Enzyme Identified in Rat Lung
Shiosaki, Kazumi,Tasker, Andrew S.,Sullivan, Gerard M.,Sorensen, Bryan K.,Geldern, Thomas W. von,et al.
, p. 468 - 478 (2007/10/02)
Two structurally distinct series of potent and selective inhibitors of an aspartyl protease-like endothelin converting enzyme (ECE) activity identified in the rat lung have been developed.Pepstatin A, which potently inhibits the rat lung ECE, served as the basis for the first series.Alternatively, selected renin inhibitors containing the dihydroxyethylene moiety were shown to be inhibitors of rat lung activity.Subsequent modifications improved inhibition of the rat lung ECE while eliminating renin activity.Both series of ECE inhibitors demonstrated a range of selectivity over Cathepsin D.Water-solubilizing moieties were appended onto selected compounds to facilitate in vivo testing.Partial reduction of the pressor response to exogenously administered Big ET-1 was observed with selected rat lung ECE inhibitors.
Nor-statine and nor-cyclostatine polypeptides
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, (2008/06/13)
Polypeptides and derivatives thereof containing nor-statine and nor-cyclostatine are useful for inhibiting the angiotensinogen-cleaving action of the enzyme renin.
