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

John N. Freskos,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

Bioorganic & Medicinal Chemistry Letters（2007）

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摘要

We describe an optimized series of acyclic hydroxyethylamine transition state isosteres of β-secretase that incorporate a variety of P2 side chains that yield potent inhibitors with excellent cellular activity and good selectivity against Cathepsin-D.

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关键词

β-Secretase,Hydroxyethylamine (HEA) isostere

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