Author/Authors :
Daisuke Shuto، نويسنده , , Soko Kasai، نويسنده , , Tooru Kimura، نويسنده , , Ping Liu، نويسنده , , Koushi Hidaka، نويسنده , , Takashi Hamada، نويسنده , , Saeko Shibakawa، نويسنده , , Yoshio Hayashi، نويسنده , , Chinatsu Hattori، نويسنده , , Beata Szabo، نويسنده , , Shoichi Ishiura، نويسنده , , Yoshiaki Kiso، نويسنده ,
Abstract :
A novel class of substrate-based β-secretase (BACE1) inhibitors containing a hydroxymethylcarbonyl (HMC) isostere was designed and synthesized. Phenylnorstatine [(2R,3S)-3-amino-2-hydroxy-4-phenylbutyric acid; Pns] was an effective transition-state mimic at the P1 position. Structure–activity relationships (SARs) of the P3–P3′ positions of BACE1 inhibitors were studied.
