888703-24-0Relevant articles and documents
Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors
Moore, Keith P.,Zhu, Hong,Rajapakse, Hemaka A.,McGaughey, Georgia B.,Colussi, Dennis,Price, Eric A.,Sankaranarayanan, Sethu,Simon, Adam J.,Pudvah, Nicole T.,Hochman, Jerome H.,Allison, Timothy,Munshi, Sanjeev K.,Graham, Samuel L.,Vacca, Joseph P.,Nantermet, Philippe G.
, p. 5831 - 5835 (2008/09/19)
This letter describes replacements for the P3 amide moiety present in previously reported tertiary carbinamine macrolactones. Although P-gp efflux issues associated with these amide-macrolactones were solved and full brain penetration was measured in one
