147 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
PMID
Data
Article Title
Organization
Design and synthesis of an orally active GPIIb/IIIa antagonist based on a phenylpiperazine scaffold.
Solvay Pharma
Design, synthesis and evaluation of novel 2-amino-3-(naphth-2-yl)propanoic acid derivatives as potent inhibitors of platelet aggregation.
China Pharmaceutical University
Synthesis, biological evaluation and molecular docking studies of 2-piperazin-1-yl-quinazolines as platelet aggregation inhibitors and ligands of integrinaIIbß3.
A.V. Bogatsky Physico-Chemical Institute Of The National Academy Of Sciences Of Ukraine
Rational improvement of the affinity and selectivity of integrin binding of grafted lasso peptides.
Philipps-Universit£T Marburg
Pharmacophoric modifications lead to superpotentavß3 integrin ligands with suppresseda5ß1 activity.
Technische Universit£T M£Nchen
Synthesis, biological evaluation, X-ray molecular structure and molecular docking studies of RGD mimetics containing 6-amino-2,3-dihydroisoindolin-1-one fragment as ligands of integrinaIIbß3.
A.V. Bogatsky Physico-Chemical Institute Of The National Academy Of Sciences Of Ukraine
Low molecular weight dual inhibitors of factor Xa and fibrinogen binding to GPIIb/IIIa with highly overlapped pharmacophores.
University Of Ljubljana
Towards dual antithrombotic compounds - balancing thrombin inhibitory and fibrinogen GPIIb/IIIa binding inhibitory activities of 2,3-dihydro-1,4-benzodioxine derivatives through regio- and stereoisomerism.
University Of Ljubljana
Biselectivity of isoDGR peptides for fibronectin binding integrin subtypesa5ß1 andavß6: conformational control through flanking amino acids.
Technische Universit£T M£Nchen
Quantitative structure-activity relationship study of fibrinogen inhibitors, [[4-(4-amidinophenoxy)butanoyl]aspartyl]valine (FK633) derivatives, using a novel hydrophobic descriptor.
Fujisawa Pharmaceutical
Three-dimensional quantitative structure-activity relationship analyses of RGD mimetics as fibrinogen receptor antagonists.
Kyoto University
Non-peptide fibrinogen receptor antagonists. 3. design and discovery of a centrally constrained inhibitor
TBA
Synthesis and solution conformation of cyclo[RGDRGD]: a cyclic peptide with selectivity for the alpha V beta 3 receptor.
Texas A&M University
Non-peptide fibrinogen receptor antagonists. 7. Design and synthesis of a potent, orally active fibrinogen receptor antagonist.
Merck Research Laboratories
Nonpeptide alpha(v)beta(3) antagonists. Part 2: constrained glycyl amides derived from the RGD tripeptide.
Merck Research Laboratories
Structure-activity relationship of a series of non peptidic RGD integrin antagonists targetinga5ß1: part 1.
Astrazeneca
alphavbeta3 Integrin-targeting Arg-Gly-Asp (RGD) peptidomimetics containing oligoethylene glycol (OEG) spacers.
Universite Catholique De Louvain
Design and synthesis of novel potent and selective integrin alphanubeta3 antagonists--novel synthetic routes to isoquinolinone, benzoxazinone, and quinazolinone acetates.
Basf
Joys of molecules. 2. Endeavors in chemical biology and medicinal chemistry.
The Scripps Research Institute
Toward a novel class of antithrombotic compounds with dual function. Discovery of 1,4-benzoxazin-3(4H)-one derivatives possessing thrombin inhibitory and fibrinogen receptor antagonistic activities.
University Of Ljubljana
Novel fibrinogen receptor antagonists. RGDF mimetics, derivatives of 4-(isoindoline-5-yl)amino-4-oxobutyric acid.
A.V. Bogatsky Physico-Chemical Institute Of The National Academy Of Sciences Of Ukraine
Design, synthesis, and biochemical evaluation of novel alpha V beta 3 integrin ligands.
3-Dimensional Pharmaceuticals
Selective alpha4beta7 integrin antagonists and their potential as antiinflammatory agents.
Genentech
Determination of the binding specificity of an integral membrane protein by saturation transfer difference NMR: RGD peptide ligands binding to integrin alphaIIbbeta3.
University Of Hamburg
Platelet glycoprotein IIb-IIIa antagonists as prototypical integrin blockers: novel parenteral and potential oral antithrombotic agents.
Cor Therapeutics
Structural analysis of thrombin complexed with potent inhibitors incorporating a phenyl group as a peptide mimetic and aminopyridines as guanidine substitutes.
3-Dimensional Pharmaceuticals
Discovery of an orally active series of isoxazoline glycoprotein IIb/IIIa antagonists.
Dupont Pharmaceuticals
Non-peptide glycoprotein IIb/IIIa inhibitors. 17. Design and synthesis of orally active, long-acting non-peptide fibrinogen receptor antagonists.
Merck Research Laboratories
Potent in vitro and in vivo inhibitors of platelet aggregation based upon the Arg-Gly-Asp sequence of fibrinogen. (Aminobenzamidino)succinyl (ABAS) series of orally active fibrinogen receptor antagonists.
Searle Research & Development
Novel thiazole-based heterocycles as selective inhibitors of fibrinogen-mediated platelet aggregation.
R. W. Johnson Pharmaceutical Research Institute
Potent inhibitors of platelet aggregation based upon the Arg-Gly-Asp-Phe sequence of fibrinogen. A proposal on the nature of the binding interaction between the Asp-carboxylate of RGDX mimetics and the platelet GP IIb-IIIa receptor.
Searle Research & Development
RGD mimetics containing a central hydantoin scaffold: alpkha(v)beta3 vs alpha(IIb)beta3 selectivity requirements.
Hoechst Marion Roussel
Synthesis, evaluation and Tc-99m complexation of a hydrazinonicotinyl conjugate of a GP IIb/IIIa antagonist cyclic peptide for the detection of deep vein thrombosis
TBA
Design, synthesis, and evaluation of fibrinogen inhibitors, -(p-amidinophenoxy) alkanoylaspartic acid derivatives
TBA
Preparation and Properties of a fibrinogen receptor antagonist containing the Arg-Gly-Asp sequence and nitroxide radicals
TBA
Tailoring of integrin ligands: probing the charge capability of the metal ion-dependent adhesion site.
Technische Universit£T M£Nchen
Fluorinated dual antithrombotic compounds based on 1,4-benzoxazine scaffold.
University Of Ljubljana
Improvement in aqueous solubility in small molecule drug discovery programs by disruption of molecular planarity and symmetry.
The University Of Tokyo
Nonpeptide GPIIb/IIIa inhibitors. 10. Centrally constrained alpha-sulfonamides are potent inhibitors of platelet aggregation
TBA
Structure-activity relationships in 3-oxo-1,4-benzodiazepine-2-acetic acid GPIIb/IIIa antagonists. The 2-benzazepine series
TBA
Solid-phase parallel synthesis applied to lead optimization: Discovery of potent analogues of the GPIIb/IIIa antagonist RWJ-50042
TBA
Non-peptide glycoprotein IIb/IIIa inhibitors. 6. Design and synthesis of rigid, centrally constrained non-peptide fibrinogen receptor antagonists
TBA
Design, synthesis and SAR of RGD peptide hybrids as highly efficient inhibitors of platelet aggregation
TBA
Synthesis and initial evaluation of novel, non-peptidic antagonists of the alpha(v)-integrins alpha(v)beta(3) and alpha(v)beta(5).
Pharmacopeia
3,4-Dihydro-2H-1,4-benzoxazine derivatives combining thrombin inhibitory and glycoprotein IIb/IIIa receptor antagonistic activity as a novel class of antithrombotic compounds with dual function.
University Of Ljubljana
Multiple N-methylation by a designed approach enhances receptor selectivity.
Technische UniversitäT MüNchen
Biphenyls as potent vitronectin receptor antagonists. Part 3: Squaric acid amides.
Bayer Healthcare
Design and synthesis of a new class of selective integrin alpha5beta1 antagonists.
Jerini
Synthesis of pyrazoles and isoxazoles as potent alpha(v)beta3 receptor antagonists.
Pfizer
Synthesis of 2,5-thiazole butanoic acids as potent and selective alpha(v)beta3 integrin receptor antagonists with improved oral pharmacokinetic properties.
Pfizer
Convergent, parallel synthesis of a series of beta-substituted 1,2,4-oxadiazole butanoic acids as potent and selective alpha(v)beta3 receptor antagonists.
Pfizer
Ligand binding analysis for human alpha5beta1 integrin: strategies for designing new alpha5beta1 integrin antagonists.
Università
Nonpeptide alpha(v)beta3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics.
Merck Research Laboratories
Design, synthesis, and biological evaluation of novel potent and selective alphavbeta3/alphavbeta5 integrin dual inhibitors with improved bioavailability. Selection of the molecular core.
Johnson And Johnson Pharmaceutical Research & Development
1,2,3,4-Tetrahydroquinoline-containing alphaVbeta3 integrin antagonists with enhanced oral bioavailability.
Johnson & Johnson Pharmaceutical Research & Development
Piperidine-containing beta-arylpropionic acids as potent antagonists of alphavbeta3/alphavbeta5 integrins.
Johnson & Johnson Pharmaceutical Research And Development
Discovery of a potent and selective alpha v beta 3 integrin antagonist with strong inhibitory activity against neointima formation in rat balloon injury model.
Dainippon Pharmaceutical
Discovery of novel 2,8-diazaspiro[4.5]decanes as orally active glycoprotein IIb-IIIa antagonists.
Millennium Pharmaceuticals
Synthesis of cinnamic acids and related isosteres as potent and selective alpha v beta 3 receptor antagonists.
Pfizer
Solid-phase synthesis of a small library of 3-phenylthio-3-nicotinyl propionic acid derivatives acting as antagonists of the integrin alphaVbeta3.
Nerviano
Synthesis and biological evaluation of nonpeptide integrin antagonists containing spirocyclic scaffolds.
Pharmaceutical Research Institute
Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis.
Merck Research Laboratories
Non-peptide alphavbeta3 antagonists. Part 6: design and synthesis of alphavbeta3 antagonists containing a pyridone or pyrazinone central scaffold.
Merck Research Laboratories
Phenylbutyrates as potent, orally bioavailable vitronectin receptor (integrin alphavbeta3) antagonists.
Glaxosmithkline
Solid-phase synthesis of cyclic RGD-furanoid sugar amino acid peptides as integrin inhibitors.
Leiden University
Highly potent and selective alphaVbeta3-receptor antagonists: solid-phase synthesis and SAR of 1-substituted 4-amino-1H-pyrimidin-2-ones.
Basf
Binding model for nonpeptide antagonists of alpha(v)beta(3) integrin.
Merck Research Laboratories
Substituted benzocyloheptenes as potent and selective alpha(v) integrin antagonists.
Institut De Recherches Servier
Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 3: synthesis and SAR of potent and specific 2,8-diazaspiro[4.5]decanes.
Cor Therapeutics
Nanomolar small molecule inhibitors for alphav(beta)6, alphav(beta)5, and alphav(beta)3 integrins.
Merck
Synthesis and SAR of N-substituted dibenzazepinone derivatives as novel potent and selective alpha(V)beta(3) antagonists.
Knoll
1,2,4-triazolo[3,4-a]pyridine as a novel, constrained template for fibrinogen receptor (GPIIb/IIIa) antagonists.
The R. W. Johnson Pharmaceutical Research Institute
alpha(v)beta(3) Antagonists based on a central thiophene scaffold.
Aventis Pharma Deutschland
Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 2: design of potent antagonists containing the 3-azaspiro[5.5]undecanes.
Cor Therapeutics
Spirocyclic nonpeptide glycoprotein IIb-IIIa antagonists. Part 1: design of potent and specific 3,9-diazaspiro[5.5]undecanes.
Cor Therapeutics
Solid-phase synthesis of a nonpeptide RGD mimetic library: new selective alphavbeta3 integrin antagonists.
Technische UniversitäT MüNchen
2-Acylimino-3H-thiazoline derivatives: a novel template for platelet GPIIb/IIIa receptor antagonists.
Taisho Pharmaceutical
Discovery of an orally active non-peptide fibrinogen receptor antagonist based on the hydantoin scaffold.
Aventis Pharma
Nonpeptide GPIIB/IIIA receptor antagonists. Part 21: C-6 flexibility and amide bond orientation are important factors in determining the affinity of compounds for activated or resting platelet receptors.
Merck Research Laboratories
Discovery and evaluation of potent, tyrosine-based alpha4beta1 integrin antagonists.
Celltech Chiroscience
Ring constrained analogues of beta-alanine-containing GPIIb/IIIa receptor antagonists.
Dupont Pharmaceuticals
Fused bicyclic Gly-Asp beta-turn mimics with potent affinity for GPIIb-IIIa. Exploration of the arginine isostere.
Eli Lilly
Selective Targeting of Integrin ?v?8 by a Highly Active Cyclic Peptide.
Technische Universit£T M£Nchen
Disubstituted indazoles as potent antagonists of the integrin alpha(v)beta(3).
Dupont Pharmaceuticals
Isoxazolines as potent antagonists of the integrin alpha(v)beta(3).
Dupont Pharmaceuticals
Discovery of orally active nonpeptide vitronectin receptor antagonists based on a 2-benzazepine Gly-Asp mimetic.
Smithkline Beecham Pharmaceuticals
Potent, orally active GPIIb/IIIa antagonists containing a nipecotic acid subunit. Structure-activity studies leading to the discovery of RWJ-53308.
The R. W. Johnson Pharmaceutical Research Institute
Fused bicyclic Gly-Asp beta-turn mimics with specific affinity for GPIIb-IIIa.
Eli Lilly
N-Methylated cyclic RGD peptides as highly active and selective alpha(V)beta(3) integrin antagonists.
Technische UniversitäT MüNchen
Orally bioavailable nonpeptide vitronectin receptor antagonists with efficacy in an osteoporosis model.
Smithkline Beecham Pharmaceuticals
Orally bioavailable nonpeptide vitronectin receptor antagonists containing 2-aminopyridine arginine mimetics.
Smithkline Beecham Pharmaceuticals
Non-peptide GPIIb/IIIa inhibitors. 20. Centrally constrained thienothiophene alpha-sulfonamides are potent, long acting in vivo inhibitors of platelet aggregation.
Merck Research Laboratories
Rapid synthesis of RGD mimetics with isoxazoline scaffolds on solid phase: identification of alphavbeta3 antagonists lead compounds.
Dupont Pharmaceuticals
Nonpeptide glycoprotein IIB/IIIA inhibitors. 19. A new design paradigm employing linearly minimized, centrally constrained, exosite inhibitors.
Merck Research Laboratories
Orally active isoxazoline glycoprotein IIb/IIIa antagonists with extended duration of action.
Dupont Pharmaceuticals
Selective, tight-binding inhibitors of integrin alpha4beta1 that inhibit allergic airway responses.
Biogen
Conformational preferences in a benzodiazepine series of potent nonpeptide fibrinogen receptor antagonists.
Smithkline Beecham Pharmaceuticals
Benzimidazole derivatives as arginine mimetics in 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonists.
Smithkline Beecham Pharmaceuticals
New platelet fibrinogen receptor glycoprotein IIb-IIIa antagonists: orally active series of N-alkylated amidines with a 6,6-bicyclic template.
Mitsui Pharmaceuticals
Design of a new class of orally active fibrinogen receptor antagonists.
RhôNe-Poulenc Rorer
GPIIb/IIIa integrin antagonists with the new conformational restriction unit, trisubstituted beta-amino acid derivatives, and a substituted benzamidine structure.
Nippon Steel
Novel non-peptide fibrinogen receptor antagonists. 1. Synthesis and glycoprotein IIb-IIIa antagonistic activities of 1,3,4-trisubstituted 2-oxopiperazine derivatives incorporating side-chain functions of the RGDF peptide.
Takeda Chemical Industries
Fibrinogen receptor (GPIIb-IIIa) antagonists derived from 5,6-bicyclic templates. Amidinoindoles, amidinoindazoles, and amidinobenzofurans containing the N-alpha-sulfonamide carboxylic acid function as potent platelet aggregation inhibitors.
Cor Therapeutics
New orally active non-peptide fibrinogen receptor (GpIIb-IIIa) antagonists: identification of ethyl 3-[N-[4-[4-[amino[(ethoxycarbonyl) imino]methyl]phenyl]-1,3-thiazol-2-yl]-N-[1-[(ethoxycarbonyl)methyl]pip erid -4-yl]amino]propionate (SR 121787) as a potent and long-acting antithrombotic agent.
Sanofi Recherche
Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists.
Eli Lilly
Discovery of potent nonpeptide vitronectin receptor (alpha v beta 3) antagonists.
Smithkline Beecham Pharmaceuticals
Non-peptide RGD surrogates which mimic a Gly-Asp beta-turn: potent antagonists of platelet glycoprotein IIb-IIIa.
Eli Lilly
From peptide to non-peptide. 3. Atropisomeric GPIIbIIIa antagonists containing the 3,4-dihydro-1H-1,4-benzodiazepine-2,5-dione nucleus.
Genentech
Discovery of potent isoxazoline glycoprotein IIb/IIIa receptor antagonists.
Dupont Pharmaceuticals
Potent, selective, orally active 3-oxo-1,4-benzodiazepine GPIIb/IIIa integrin antagonists.
Smithkline Beecham Pharmaceuticals
Orally active fibrinogen receptor antagonists. 2. Amidoximes as prodrugs of amidines.
F. Hoffmann-La Roche
Design, synthesis of novel tryptophan derivatives for antiplatelet aggregation activity based on tripeptide pENW (pGlu-Asn-Trp).
China Pharmaceutical University
Strategies to inhibit tumor associated integrin receptors: rationale for dual and multi-antagonists.
University Of Bradford
Conformationally constrained peptides and semipeptides derived from RGD as potent inhibitors of the platelet fibrinogen receptor and platelet aggregation.
Smithkline Beecham Pharmaceuticals Research And Development
Non-peptide fibrinogen receptor antagonists. 2. Optimization of a tyrosine template as a mimic for Arg-Gly-Asp.
Merck Research Laboratories
Potent non-peptide fibrinogen receptor antagonists which present an alternative pharmacophore.
Smithkline Beecham Pharmaceuticals
Design and evaluation of nonpeptide fibrinogen gamma-chain based GPIIb/IIIa antagonists.
R. W. Johnson Pharmaceutical Research Institute
Design and synthesis of novel cyclic RGD-containing peptides as highly potent and selective integrin alpha IIb beta 3 antagonists.
Telios Pharmaceuticals
Drug-target interactions that involve the replacement or displacement of magnesium ions.
Bristol-Myers Squibb Research And Development
Emergence of Small-Molecule Non-RGD-Mimetic Inhibitors for RGD Integrins.
University Of Strathclyde
Development of a small RGD peptide fibrinogen receptor antagonist with potent antiaggregatory activity in vitro.
Smithkline Beecham Pharmaceuticals Research And Development
Natural-Products-Inspired Use of the gem-Dimethyl Group in Medicinal Chemistry.
St. John'S University
Non-peptide fibrinogen receptor antagonists. 1. Discovery and design of exosite inhibitors.
Merck Research Laboratories
Design and synthesis of a C7 mimetic for the predicted gamma-turn conformation found in several constrained RGD antagonists.
Smithkline Beecham Pharmaceuticals
Investigation of conformational specificity at GPIIb/IIIa: evaluation of conformationally constrained RGD peptides.
Smithkline Beecham Pharmaceuticals
