Author/Authors :
Marcus B?ck، نويسنده , , Jonas Nyhlén، نويسنده , , Ingemar Kvarnstr?m، نويسنده , , Sara Appelgren، نويسنده , , Neera Borkakoti، نويسنده , , Katarina Jansson، نويسنده , , Jimmy Lindberg، نويسنده , , Susanne Nystr?m، نويسنده , , Anders Hallberg، نويسنده , , Asa Rosenquist، نويسنده , , Bertil Samuelsson، نويسنده ,
Abstract :
Several BACE-1 inhibitors with low nanomolar level activities, encompassing a statine-based core structure with phenyloxymethyl- and benzyloxymethyl residues in the P1 position, are presented. The novel P1 modification introduced to allow the facile exploration of the S1 binding pocket of BACE-1, delivered highly promising inhibitors.
Keywords :
Alzheimer’s disease , BACE-1 inhibitors , P1 modifications , peptidomimetics