913626-08-1Relevant articles and documents
Macrocyclic inhibitors of β-secretase: Functional activity in an animal model
Stachel, Shawn J.,Coburn, Craig A.,Sankaranarayanan, Sethu,Price, Eric A.,Pietrak, Beth L.,Huang, Qian,Lineberger, Janet,Espeseth, Amy S.,Jin, Lixia,Ellis, Joan,Holloway, M. Katharine,Munshi, Sanjeev,Allison, Timothy,Hazuda, Daria,Simon, Adam J.,Graham, Samuel L.,Vacca, Joseph P.
, p. 6147 - 6150 (2006)
A macrocyclic inhibitor of β-secretase was designed by covalently cross-linking the P1 and P3 side chains of an isophthalamide-based inhibitor. Macrocyclization resulted in significantly improved potency and physical properties when compared to the initia