Freskos John N, Fobian Yvette M, Benson Timothy E, Bienkowski Michael J, Brown David L, Emmons Thomas L, Heintz Robert, Laborde Alice, McDonald Joseph J, Mischke Brent V, Molyneaux John M, Moon Joseph B, Mullins Patrick B, Bryan Prince D, Paddock Donna J, Tomasselli Alfredo G, Winterrowd Gregory
Pfizer Inc., 700N. Chesterfield Pkwy., St. Louis, MO 63198, USA.
Bioorg Med Chem Lett. 2007 Jan 1;17(1):73-7. doi: 10.1016/j.bmcl.2006.09.092. Epub 2006 Oct 4.
We describe a novel series of potent inhibitors of human beta-secretase. These compounds possess the hydroxyethyl amine transition state isostere. A 2.5A crystal structure of inhibitor 32 bound to BACE is provided.
我们描述了一系列新型的人类β-分泌酶强效抑制剂。这些化合物具有羟乙胺过渡态类似物。提供了与β-分泌酶(BACE)结合的抑制剂32的2.5埃晶体结构。