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

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

Bioorganic & Medicinal Chemistry Letters（2007）

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摘要

We describe a novel series of potent inhibitors of human β-secretase. These compounds possess the hydroxyethyl amine transition state isostere. A 2.5Å crystal structure of inhibitor 32 bound to BACE is provided.

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关键词

β-Secretase,Hydroxyethylamine (HEA) isostere

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