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PDBsum entry 3iit
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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 cis-1,2-Diaminocyclohexane derivatives as potent factor xa inhibitors. Part ii: exploration of 6-6 fused rings as alternative s1 moieties.
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Authors
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K.Yoshikawa,
S.Kobayashi,
Y.Nakamoto,
N.Haginoya,
S.Komoriya,
T.Yoshino,
T.Nagata,
A.Mochizuki,
K.Watanabe,
M.Suzuki,
H.Kanno,
T.Ohta.
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Ref.
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Bioorg Med Chem Lett, 2009,
17,
8221-8233.
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PubMed id
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Abstract
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A series of cis-1,2-diaminocyclohexane derivatives possessing a 6-6 fused ring
for the S1 moiety were synthesized as novel factor Xa (fXa) inhibitors. The
synthesis, structure-activity relationship (SAR), and physicochemical properties
are reported herein, together with the discovery of compound 45c, which has
potent anti-fXa activity, good physicochemical properties and pharmacokinetic
(PK) profiles, including a reduced negative food effect.
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