PMID

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Article Title

Organization

Development of Potent and Selective Antagonists for the UTP-Activated P2Y

University of Bonn

Identification of Highly Promising Antioxidants/Neuroprotectants Based on Nucleoside 5'-Phosphorothioate Scaffold. Synthesis, Activity, and Mechanisms of Action.

Bar-Ilan University

Discovery of 4-aryl-7-hydroxyindoline-based P2Y1 antagonists as novel antiplatelet agents.

Bristol-Myers Squibb Research

Highly potent and selective ectonucleotide pyrophosphatase/phosphodiesterase I inhibitors based on an adenosine 5'-(a or¿)-thio-(a,ß- orß,¿)-methylenetriphosphate scaffold.

Bar-Ilan University

Identification of 1-{2-[4-chloro-1'-(2,2-dimethylpropyl)-7-hydroxy-1,2-dihydrospiro[indole-3,4'-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3]thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y(1) antagonist as an antiplatelet agent.

Bristol-Myers Squibb

2-Amino-1,3,4-thiadiazoles in the 7-hydroxy-N-neopentyl spiropiperidine indolinyl series as potent P2Y1 receptor antagonists.

Bristol-Myers Squibb

Conformationally constrained ortho-anilino diaryl ureas: discovery of 1-(2-(1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenyl)-3-(4-(trifluoromethoxy)phenyl)urea, a potent, selective, and bioavailable P2Y1 antagonist.

Bristol-Myers Squibb

Potent P2Y1 urea antagonists bearing various cyclic amine scaffolds.

Bristol-Myers Squibb

Design, synthesis and structure-activity relationships of zwitterionic spirocyclic compounds as potent CCR1 antagonists.

Astrazeneca

2-Aminothiazole based P2Y(1) antagonists as novel antiplatelet agents.

Bristol-Myers Squibb

New azole antagonists with high affinity for the P2Y(1) receptor.

Bristol-Myers Squibb

Highly efficient biocompatible neuroprotectants with dual activity as antioxidants and P2Y receptor agonists.

Bar-Ilan University

Discovery of diarylurea P2Y(1) antagonists with improved aqueous solubility.

Bristol-Myers Squibb

Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists.

Bristol-Myers Squibb Research and Development

Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potency.

University of Bonn

Identification of high-affinity P2Y12 antagonists based on a phenylpyrazole glutamic acid piperazine backbone.

Sanofi-Aventis Deutschland

Virtual screening leads to the discovery of novel non-nucleotide P2Y1 receptor antagonists.

National Institutes of Health

Benzofuran-substituted urea derivatives as novel P2Y(1) receptor antagonists.

Glaxosmithkline

P2Y1 receptor antagonists as novel antithrombotic agents.

Pfizer

Lipophilic modifications to dinucleoside polyphosphates and nucleotides that confer antagonist properties at the platelet P2Y12 receptor.

Inspire Pharmaceuticals

Novel nucleotide triphosphates as potent P2Y2 agonists with enhanced stability over UTP.

Ucb-Group

Novel nucleotide triphosphates as potent P2Y2 agonists.

Ucb-Group

Diadenosine and diuridine poly(borano)phosphate analogues: synthesis, chemical and enzymatic stability, and activity at P2Y1 and P2Y2 receptors.

Bar-Ilan University

Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.

National Institute of Diabetes and Digestive and Kidney Diseases

Novel antagonists acting at the P2Y(1) purinergic receptor: synthesis and conformational analysis using potentiometric and nuclear magnetic resonance titration techniques.

Universit£

Purine and pyrimidine (P2) receptors as drug targets.

National Institute of Diabetes

Adenine nucleotide analogues locked in a Northern methanocarba conformation: enhanced stability and potency as P2Y(1) receptor agonists.

National Institute of Diabetes

Methanocarba modification of uracil and adenine nucleotides: high potency of Northern ring conformation at P2Y1, P2Y2, P2Y4, and P2Y11 but not P2Y6 receptors.

National Institute of Diabetes

Human P2Y1 receptor: molecular modeling and site-directed mutagenesis as tools to identify agonist and antagonist recognition sites.

National Institute of Diabetes

Diadenosine 5',5''-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors.

Bar-Ilan University

Frontal affinity chromatography-mass spectrometry useful for characterization of new ligands for GPR17 receptor.

University of Pavia

Structure-activity relationship of (N)-Methanocarba phosphonate analogues of 5'-AMP as cardioprotective agents acting through a cardiac P2X receptor.

National Institutes of Diabetes and Digestive and Kidney Diseases

A novel insulin secretagogue based on a dinucleoside polyphosphate scaffold.

Bar-Ilan University

Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists.

Glaxosmithkline

P2Y1 antagonists: combining receptor-based modeling and QSAR for a quantitative prediction of the biological activity based on consensus scoring.

National Institute of Diabetes and Digestive and Kidney Diseases

3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.

Glaxosmithkline

Discovery of a Series of 5-Amide-1

China Pharmaceutical University

Progress of thrombus formation and research on the structure-activity relationship for antithrombotic drugs.

Northwest University

P2Y

Al-Ahliyya Amman University

2-Substitution of adenine nucleotide analogues containing a bicyclo[3.1.0]hexane ring system locked in a northern conformation: enhanced potency as P2Y1 receptor antagonists.

Niddk

Structure-Based Design of 3-(4-Aryl-1H-1,2,3-triazol-1-yl)-Biphenyl Derivatives as P2Y14 Receptor Antagonists.

National Institute of Diabetes and Digestive and Kidney Diseases

New highly active antiplatelet agents with dual specificity for platelet P2Y1 and P2Y12 adenosine diphosphate receptors.

Glsynthesis

New iantherans from the marine sponge Ianthella quadrangulata: novel agonists of the P2Y(11) receptor.

University of Bonn

Design, synthesis, and biological evaluation of 2-(phenoxyaryl)-3-urea derivatives as novel P2Y

University of Chinese Academy of Sciences

Current knowledge on the nucleotide agonists for the P2Y2 receptor.

China Pharmaceutical University

Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-? Inhibitors.

Pharmaron-Beijing

Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease.

Yogi Vemana University

Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b.

University of Leipzig

Synthesis and evaluation of 2-pyridinone derivatives as specific HIV-1 reverse transcriptase inhibitors. 3. Pyridyl and phenyl analogs of 3-aminopyridin-2(1H)-one.

Merck Research Laboratories