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PDBsum entry 3nsh
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References listed in PDB file
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Key reference
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Title
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Design and synthesis of hydroxyethylamine (hea) bace-1 inhibitors: structure-Activity relationship of the aryl region.
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Authors
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G.D.Probst,
S.Bowers,
J.M.Sealy,
B.Stupi,
D.Dressen,
B.M.Jagodzinska,
J.Aquino,
A.Gailunas,
A.P.Truong,
L.Tso,
Y.Z.Xu,
R.K.Hom,
V.John,
J.S.Tung,
M.A.Pleiss,
J.A.Tucker,
A.W.Konradi,
H.L.Sham,
J.Jagodzinski,
G.Toth,
E.Brecht,
N.Yao,
H.Pan,
M.Lin,
D.R.Artis,
L.Ruslim,
M.P.Bova,
S.Sinha,
T.A.Yednock,
S.Gauby,
W.Zmolek,
K.P.Quinn,
J.M.Sauer.
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Ref.
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Bioorg Med Chem Lett, 2010,
20,
6034-6039.
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PubMed id
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Abstract
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The structure-activity relationship of the prime region of hydroxyethylamine
BACE inhibitors is described. Variation in the aryl linker region with 5- and
6-membered heterocycles provided compounds such as 33 with improved permeability
and reduced P-gp liability compared to benzyl amine analog 1.
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