Orally efficacious thrombin inhibitors with cyanofluorophenylacetamide as the P2 motif (original) (raw)

Discovery of potent, selective 4-fluoroproline-based thrombin inhibitors with improved metabolic stability

Sean Yu

Bioorganic & Medicinal Chemistry, 2006

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Design and structure–activity relationship of thrombin inhibitors with an azaphenylalanine scaffold: potency and selectivity enhancements via P2 optimization

Gregor Mlinsek

Bioorganic & Medicinal Chemistry, 2001

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New Synthetic Thrombin Inhibitors: Molecular Design and Experimental Verification

alexey romanov

PLoS ONE, 2011

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Structure of a novel thrombin inhibitor with an uncharged d-amino acid as P1 residue

Peter Goettig

European Journal of Medicinal Chemistry, 2008

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Discovery of a Novel, Selective, and Orally Bioavailable Class of Thrombin Inhibitors Incorporating Aminopyridyl Moieties at the P1 Position

Joseph Vacca

Journal of Medicinal Chemistry, 1997

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In vitro evaluation and crystallographic analysis of a new class of selective, non-amide-based thrombin inhibitors

richard soll

Bioorganic & Medicinal Chemistry Letters, 1998

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Rational Design and Characterization of D-Phe-Pro-D-Arg-Derived Direct Thrombin Inhibitors

Juliane Barbosa

PLOS One, 2012

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Structure–activity and crystallographic analysis of a new class of non-amide-based thrombin inhibitor

richard soll

Bioorganic & Medicinal Chemistry Letters, 2000

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Thrombin inhibitor design: X-ray and solution studies provide a novel P1 determinant

Lawrence Berliner

Journal of protein chemistry, 2000

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Novel Potent and Selective Thrombin Inhibitors Based on a Central 1,4-Benzoxazin-3(4 H )-one Scaffold △

Janez Ilaš

Journal of Medicinal Chemistry, 2008

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Design of Weakly Basic Thrombin Inhibitors Incorporating Novel P1 Binding Functions: Molecular and X-ray Crystallographic Studies

Giuseppina Simone

Biochemistry, 2003

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Structure-Based Design of Residue 1 Analogs of the Direct Thrombin Inhibitor Pentapeptide FM 19

Henry I. Mosberg

Chemical Biology & Drug Design, 2010

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Crystal structure of two new bifunctional nonsubstrate type thrombin inhibitors complexed with human α-thrombin

james fethiere

Protein Science, 2008

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Discovery and Clinical Evaluation of 1-{ N -[2-(Amidinoaminooxy)ethyl]amino}carbonylmethyl-6-methyl-3-[2,2-difluoro-2-phenylethylamino]pyrazinone (RWJ-671818), a Thrombin Inhibitor with an Oxyguanidine P1 Motif

Bruce Damiano

Journal of Medicinal Chemistry, 2010

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P2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold

Joseph Vacca

Bioorganic & Medicinal Chemistry Letters, 2005

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2-(2-Chloro-6-fluorophenyl)acetamides as potent thrombin inhibitors

Bruce Tomczuk

Bioorganic & Medicinal Chemistry Letters, 2007

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Structure-Based Design and Structure-Activity Relationships of D-Phe-Pro-D-Arg-P1′-CONH2 Tetrapeptides Inhibitors of Thrombin

ziqian wang

Understanding Biology Using Peptides

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Progress in the design of low molecular weight thrombin inhibitors

Dinesh Dikshit

Medicinal Research Reviews, 2005

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Rational design of selective thrombin inhibitors

Sangsoo Kim

Bioorganic & Medicinal Chemistry Letters, 1997

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Technical Scale Synthesis of a New and Highly Potent Thrombin Inhibitor

Bernd Schaefer

Synthesis, 2004

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SSR182289A, a selective and potent orally active thrombin inhibitor

gilbert lassalle

Bioorganic & Medicinal Chemistry, 2004

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Synthesis and Biological Evaluation of Direct Thrombin Inhibitors Bearing 4-(Piperidin-1-yl)pyridine at the P1 Position with Potent Anticoagulant Activity

C. Altomare

Journal of Medicinal Chemistry, 2013

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Design and synthesis of potent and selective macrocyclic thrombin inhibitors

Joseph Vacca

Bioorganic & Medicinal Chemistry Letters, 2003

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Unexpected enhancement of thrombin inhibitor potency with o-aminoalkylbenzylamides in the P1 position

Joseph Vacca

Bioorganic & Medicinal Chemistry Letters, 2003

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Thrombin inhibitors identified by computer-assisted multiparameter design

Christian Merkwirth

Proceedings of the …, 2005

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Structure-Based Design, Synthesis and Evaluation of Novel Peptidic Inhibitors of Thrombin-Induced Activation of Platelets Aggregation

Manfred Philipp

2015

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Send Orders for Reprints to reprints@benthamscience.net Pharmacophore Design, Virtual Screening, Molecular Docking and Optimization Approaches to Discover Potent Thrombin Inhibitors

Meganathan Chandrasekaran

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