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PDBsum entry 2ei6
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References listed in PDB file
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Key reference
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Title
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Cycloalkanediamine derivatives as novel blood coagulation factor xa inhibitors.
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Authors
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T.Nagata,
T.Yoshino,
N.Haginoya,
K.Yoshikawa,
Y.Isobe,
T.Furugohri,
H.Kanno.
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Ref.
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Bioorg Med Chem Lett, 2007,
17,
4683-4688.
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PubMed id
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Abstract
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This paper describes the synthesis of orally available potent fXa inhibitors 2
and 3 by modification of the piperazine part of lead compound 1. Carbonyl
derivative 3 showed potent fXa activity but not sulfonyl derivative 2. Among the
compounds synthesized, cyclohexane derivatives 3g and 3h and cycloheptane
derivative 3j had potent anticoagulant activity as well as anti-fXa activity.
Synthetic study of the optical isomers of 3g demonstrated that (-)-3g had more
potent activity.
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