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PDBsum entry 4jzd
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Hydrolase/hydrolase inhibitor
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PDB id
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4jzd
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References listed in PDB file
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Key reference
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Title
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Discovery of nonbenzamidine factor viia inhibitors using a biaryl acid scaffold.
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Authors
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S.A.Bolton,
J.C.Sutton,
R.Anumula,
G.S.Bisacchi,
B.Jacobson,
W.A.Slusarchyk,
U.D.Treuner,
S.C.Wu,
G.Zhao,
Z.Pi,
S.Sheriff,
R.A.Smirk,
S.Bisaha,
D.L.Cheney,
A.Wei,
W.A.Schumacher,
K.S.Hartl,
E.Liu,
R.Zahler,
S.M.Seiler.
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Ref.
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Bioorg Med Chem Lett, 2013,
23,
5239-5243.
[DOI no: ]
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PubMed id
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Abstract
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In this Letter, we describe the synthesis of several nonamidine analogs of
biaryl acid factor VIIa inhibitor 1 containing weakly basic or nonbasic P1
groups. 2-Aminoisoquinoline was found to be an excellent surrogate for the
benzamidine group (compound 2) wherein potent inhibition of factor VIIa is
maintained relative to most other related serine proteases. In an unanticipated
result, the m-benzamide P1 (compounds 21a and 21b) proved to be a viable
benzamidine replacement, albeit with a 20-40 fold loss in potency against factor
VIIa.
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