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PDBsum entry 2cji
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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 and synthesis of orally active pyrrolidin-2-One-Based factor xa inhibitors.
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Authors
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N.S.Watson,
D.Brown,
M.Campbell,
C.Chan,
L.Chaudry,
M.A.Convery,
R.Fenwick,
J.N.Hamblin,
C.Haslam,
H.A.Kelly,
N.P.King,
C.L.Kurtis,
A.R.Leach,
G.R.Manchee,
A.M.Mason,
C.Mitchell,
C.Patel,
V.K.Patel,
S.Senger,
G.P.Shah,
H.E.Weston,
C.Whitworth,
R.J.Young.
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Ref.
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Bioorg Med Chem Lett, 2006,
16,
3784-3788.
[DOI no: ]
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PubMed id
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Abstract
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A series of novel, non-basic
3-(6-chloronaphth-2-ylsulfonyl)aminopyrrolidin-2-one-based factor Xa (fXa)
inhibitors, incorporating an alanylamide P4 group, was designed and synthesised.
Within this series, the N-2-(morpholin-4-yl)-2-oxoethyl derivative 24 was shown
to be a potent, selective fXa inhibitor with good anticoagulant activity.
Moreover, 24 possessed highly encouraging rat and dog pharmacokinetic profiles
with excellent oral bioavailabilities in both species.
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