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PDBsum entry 2ph6
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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, Synthesis, And sar of macrocyclic tertiary carbinamine bace-1 inhibitors.
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Authors
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S.R.Lindsley,
K.P.Moore,
H.A.Rajapakse,
H.G.Selnick,
M.B.Young,
H.Zhu,
S.Munshi,
L.Kuo,
G.B.Mcgaughey,
D.Colussi,
M.C.Crouthamel,
M.T.Lai,
B.Pietrak,
E.A.Price,
S.Sankaranarayanan,
A.J.Simon,
G.R.Seabrook,
D.J.Hazuda,
N.T.Pudvah,
J.H.Hochman,
S.L.Graham,
J.P.Vacca,
P.G.Nantermet.
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Ref.
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Bioorg Med Chem Lett, 2007,
17,
4057-4061.
[DOI no: ]
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PubMed id
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Abstract
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This Letter describes the design and synthesis of tertiary carbinamine
macrocyclic inhibitors of the beta-secretase (BACE-1) enzyme. These macrocyclic
inhibitors, some of which incorporate novel P2 substituents, display a 2- to
100-fold increase in potency relative to the previously described acyclic
analogs while affording greater stability.
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