1067651-28-8Relevant articles and documents
Design and synthesis of potent and selective BACE-1 inhibitor
Bj?rklund, Catarina,Oscarson, Stefan,Benkestock, Kurt,Borkakoti, Neera,Jansson, Katarina,Lindberg, Jimmy,Vrang, Lotta,Hallberg, Anders,Rosenquist, Asa,Samuelsson, Bertil
experimental part, p. 1458 - 1464 (2010/08/03)
Highly potent BACE-1 protease inhibitors have been developed from an inhibitors containing a hydroxyethylene (HE) core displaying aryloxymethyl or benzyloxymethyl P1 side chain and a methoxy P1′ side chain. The target molecules were synthesized in good overall yields from chiral carbohydrate starting materials. The inhibitors show high BACE-1 potency and good, selectivity against cathepsin D, where the most potent inhibitor furnishes BACE-1 Ki ? 1 nM and displays > 1000-fold selectivity over cathepsin D.