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PDBsum entry 4ryc
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Hydrolase/hydrolase inhibitor
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PDB id
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4ryc
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References listed in PDB file
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Key reference
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Title
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Trans-(3s,4s)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part i: prime site exploration using an amino linker.
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Authors
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E.Lorthiois,
F.Cumin,
C.Ehrhardt,
T.Kosaka,
H.Sellner,
N.Ostermann,
E.Francotte,
T.Wagner,
J.Maibaum.
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Ref.
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Bioorg Med Chem Lett, 2015,
25,
1782-1786.
[DOI no: ]
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PubMed id
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Abstract
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Recently, we reported on the discovery of (3S,4S)-disubstituted pyrrolidines
(e.g., 2) as inhibitors of the human aspartyl protease renin. In our effort to
further expand the scope of this novel class of direct renin inhibitors, a new
sub-series was designed in which the prime site substituents are linked to the
pyrrolidine core by a (3S)-amino functional group. In particular, analogs
bearing the corresponding sulfonamide spacer (50, 51 and 54a) demonstrated a
pronounced increase in in vitro potency compared to compound 2.
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