人β-分泌酶强效抑制剂的设计。第2部分。
Design of potent inhibitors of human beta-secretase. Part 2.
作者信息
Freskos John N, Fobian Yvette M, Benson Timothy E, Moon Joseph B, Bienkowski Michael J, Brown David L, Emmons Thomas L, Heintz Robert, Laborde Alice, McDonald Joseph J, Mischke Brent V, Molyneaux John M, Mullins Patrick B, Bryan Prince D, Paddock Donna J, Tomasselli Alfredo G, Winterrowd Greg
机构信息
Pfizer Inc., 700N. Chesterfield Pkwy., St. Louis, MO 63198, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jan 1;17(1):78-81. doi: 10.1016/j.bmcl.2006.09.091. Epub 2006 Oct 4.
We describe an optimized series of acyclic hydroxyethylamine transition state isosteres of beta-secretase that incorporates a variety of P(2) side chains that yield potent inhibitors with excellent cellular activity. A 2.2A crystal structure of compound 13 is shown.
我们描述了一系列经过优化的β-分泌酶的无环羟乙胺过渡态类似物，其中包含多种P(2)侧链，这些侧链可产生具有出色细胞活性的强效抑制剂。展示了化合物13的2.2埃晶体结构。
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