National Center for
4I1C: Design And Synthesis Of Thiophene Dihydroisoquinolins As Novel Bace-1 Inhibitors
Bioorg. Med. Chem. Lett. (2013) 23 p.3075-3080
Utilizing a structure based design approach, combined with extensive medicinal chemistry execution, highly selective, potent and novel BACE1 inhibitor 8 (BACE1 Alpha assay IC50=8nM) was made from a weak muM potency hit in an extremely efficient way. The detailed SAR and general design approaches will be discussed.