Design of potent inhibitors of human β-secretase.: Part 1

被引：39

作者：

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.

Prince, D. Bryan

Paddock, Donna J.

Tomasselli, Alfredo G.

Winterrowd, Gregory

机构：

[1] Pfizer Inc, St Louis, MO 63198 USA

[2] Pfizer Inc, Ann Arbor, MI 48105 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 01期

关键词：

beta-Secretase; hydroxyethylamine (HEA) isostere;

D O I：

10.1016/j.bmcl.2006.09.092

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We describe a novel series of potent inhibitors of human beta-secretase. These compounds possess the hydroxyethyl amine transition state isostere. A 2.5 angstrom crystal structure of inhibitor 32 bound to BACE is provided. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：73 / 77

页数：5

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