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PDBsum entry 3f8s
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References listed in PDB file
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Key reference
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Title
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(3,3-Difluoro-Pyrrolidin-1-Yl)-[(2s,4s)-(4-(4-Pyrimidin-2-Yl-Piperazin-1-Yl)-Pyrrolidin-2-Yl]-Methanone: a potent, Selective, Orally active dipeptidyl peptidase iv inhibitor.
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Authors
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M.J.Ammirati,
K.M.Andrews,
D.D.Boyer,
A.M.Brodeur,
D.E.Danley,
S.D.Doran,
B.Hulin,
S.Liu,
R.K.Mcpherson,
S.J.Orena,
J.C.Parker,
J.Polivkova,
X.Qiu,
C.B.Soglia,
J.L.Treadway,
M.A.Vanvolkenburg,
D.C.Wilder,
D.W.Piotrowski.
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Ref.
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Bioorg Med Chem Lett, 2009,
19,
1991-1995.
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PubMed id
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Abstract
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A series of 4-substituted proline amides was synthesized and evaluated as
inhibitors of dipeptidyl pepdidase IV for the treatment of type 2 diabetes.
(3,3-Difluoro-pyrrolidin-1-yl)-[(2S,4S)-(4-(4-pyrimidin-2-yl-piperazin-1-yl)-pyrrolidin-2-yl]-methanone
(5) emerged as a potent (IC(50) = 13 nM) and selective compound, with high oral
bioavailability in preclinical species and low plasma protein binding. Compound
5, PF-00734200, was selected for development as a potential new treatment for
type 2 diabetes.
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