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PDBsum entry 2g00
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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 potent, Efficacious, And orally bioavailable inhibitors of blood coagulation factor xa with neutral p1 moieties.
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Authors
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D.J.Pinto,
R.A.Galemmo,
M.L.Quan,
M.J.Orwat,
C.Clark,
R.Li,
B.Wells,
F.Woerner,
R.S.Alexander,
K.A.Rossi,
A.Smallwood,
P.C.Wong,
J.M.Luettgen,
A.R.Rendina,
R.M.Knabb,
K.He,
R.R.Wexler,
P.Y.Lam.
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Ref.
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Bioorg Med Chem Lett, 2006,
16,
5584-5589.
[DOI no: ]
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PubMed id
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Abstract
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The bicyclic dihydropyrazolopyridinone scaffold allowed for incorporation of
multiple P1 moieties with subnanomolar binding affinities for blood coagulation
factor Xa. The compound
3-[6-(2'-dimethylaminomethyl-biphenyl-4-yl)-7-oxo-3-trifluoro-methyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridine-l-yl]-benzamide
6d shows good fXa potency, selectivity, in vivo efficacy and oral
bioavailability. Compound 6d was selected for further pre-clinical evaluations.
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