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PDBsum entry 2uwp
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References listed in PDB file
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Key reference
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Title
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Selective and dual action orally active inhibitors of thrombin and factor xa.
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Authors
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R.J.Young,
D.Brown,
C.L.Burns-Kurtis,
C.Chan,
M.A.Convery,
J.A.Hubbard,
H.A.Kelly,
A.J.Pateman,
A.Patikis,
S.Senger,
G.P.Shah,
J.R.Toomey,
N.S.Watson,
P.Zhou.
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Ref.
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Bioorg Med Chem Lett, 2007,
17,
2927-2930.
[DOI no: ]
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PubMed id
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Abstract
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The synthetic entry to new classes of dual fXa/thrombin and selective thrombin
inhibitors with significant oral bioavailability is described. This was achieved
through minor modifications to the sulfonamide group in our potent and selective
fXa inhibitor
(E)-2-(5-chlorothien-2-yl)-N-{(3S)-1-[(1S)-1-methyl-2-(morpholin-4-yl)-2-oxoethyl]-2-oxopyrrolidin-3-yl}ethenesulfonamide
and these observed activity changes have been rationalised using structural
studies.
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