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. 2007 Jan 1;17(1):78-81.
doi: 10.1016/j.bmcl.2006.09.091. Epub 2006 Oct 4.

Design of potent inhibitors of human beta-secretase. Part 2

John N Freskos  1 , Yvette M Fobian, Timothy E Benson, Joseph B Moon, Michael J Bienkowski, David L Brown, Thomas L Emmons, Robert Heintz, Alice Laborde, Joseph J McDonald, Brent V Mischke, John M Molyneaux, Patrick B Mullins, D Bryan Prince, Donna J Paddock, Alfredo G Tomasselli, Greg Winterrowd
Affiliations

Design of potent inhibitors of human beta-secretase. Part 2

John N Freskos et al. Bioorg Med Chem Lett. .

Abstract

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.

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