856875-41-7Relevant academic research and scientific papers
Design and synthesis of 5,5′-disubstituted aminohydantoins as potent and selective human β-secretase (BACE1) inhibitors
Malamas, Michael S.,Erdei, Jim,Gunawan, Iwan,Turner, Jim,Hu, Yun,Wagner, Erik,Fan, Kristi,Chopra, Rajiv,Olland, Andrea,Bard, Jonathan,Jacobsen, Steve,Magolda, Ronald L.,Pangalos, Menelas,Robichaud, Albert J.
experimental part, p. 1146 - 1158 (2010/07/02)
The identification of small molecule aminohydantoins as potent and selective human β-secretase inhibitors is reported. These analogues exhibit low nannomolar potency for BACE1, show comparable activity in a cell-based (ELISA) assay, and demonstrate 50 value for BACE1 of 10 nM and exhibited comparable cellular activity (EC 50 = 20 nM) in the ELISA assay. Acute oral administration of (S)-55 at 100 mg/kg resulted in a 69% reduction of plasma Aβ40 at 8 h in a Tg2576 mouse (p 0.001).
