195 articles for thisTarget
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Article Title
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Discovery and pharmacological evaluation of a novel series of adamantyl cyanoguanidines as P2X
The University of Sydney
Development of Potent and Selective Antagonists for the UTP-Activated P2Y
University of Bonn
Escape from adamantane: Scaffold optimization of novel P2X7 antagonists featuring complex polycycles.
Universitat De Barcelona
The discovery and preclinical characterization of 6-chloro-N-(2-(4,4-difluoropiperidin-1-yl)-2-(2-(trifluoromethyl)pyrimidin-5-yl)ethyl)quinoline-5-carboxamide based P2X7 antagonists.
Janssen Research and Development
Identification of (R)-(2-Chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyridin-2-yl)-4-methyl-6,7-dihydro-1H-imidazo[4,5-c]pyridin-5(4H)-yl)methanone (JNJ 54166060), a Small Molecule Antagonist of the P2X7 receptor.
Janssen Research and Development
Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists.
Janssen Research and Development
Identification of Highly Promising Antioxidants/Neuroprotectants Based on Nucleoside 5'-Phosphorothioate Scaffold. Synthesis, Activity, and Mechanisms of Action.
Bar-Ilan University
Novel methyl substituted 1-(5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)methanones are P2X7 antagonists.
Janssen Research and Development
Docking of competitive inhibitors to the P2X7 receptor family reveals key differences responsible for changes in response between rat and human.
University of Leeds
Discovery of novel 2,5-dioxoimidazolidine-based P2X(7) receptor antagonists as constrained analogues of KN62.
Gwangju Institute of Science and Technology (Gist)
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 and synthesis of potent and selective P2X3 receptor antagonists derived from PPADS as potential pain modulators.
Gwangju Institute of Science and Technology (Gist)
Flow Synthesis and Biological Studies of an Analgesic Adamantane Derivative That Inhibits P2X7-Evoked Glutamate Release.
University of Cambridge
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
Evaluation of adenine as scaffold for the development of novel P2X3 receptor antagonists.
University of Camerino
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
Synthesis and structure-activity relationships of carboxylic acid derivatives of pyridoxal as P2X receptor antagonists.
Gwangju Institute of Science and Technology
Discovery of 2-(phenoxypyridine)-3-phenylureas as small molecule P2Y1 antagonists.
Bristol-Myers Squibb Research and Development
Synthesis and Pharmacological Characterization of Two Novel, Brain Penetrating P2X7 Antagonists.
Janssen Research and Development
Novel and potent 3-(2,3-dichlorophenyl)-4-(benzyl)-4H-1,2,4-triazole P2X7 antagonists.
Abbott Laboratories
Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potency.
University of Bonn
Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine P2X(7) antagonists.
Abbott Laboratories
Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X(7) receptor.
Glaxosmithkline
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.
Glaxosmithkline
Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor.
Glaxosmithkline
Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor.
Glaxosmithkline
Discovery and optimization of RO-85, a novel drug-like, potent, and selective P2X3 receptor antagonist.
Roche Palo Alto
Antagonists of the P2X(7) receptor. From lead identification to drug development.
Astrazeneca
Discovery and biological evaluation of novel cyanoguanidine P2X(7) antagonists with analgesic activity in a rat model of neuropathic pain.
Abbott Laboratories
Structure-activity relationship studies on N'-aryl carbohydrazide P2X7 antagonists.
Abbott Laboratories
Synthesis and in vitro activity of 1-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-1H-1,2,4-triazol-5-amine and 4-(2,3-dichlorophenyl)-N-(pyridin-3-ylmethyl)-4H-1,2,4-triazol-3-amine P2X7 antagonists.
Abbott Laboratories
Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
Abbott Laboratories
N-substituted phenoxazine and acridone derivatives: structure-activity relationships of potent P2X4 receptor antagonists.
University of Bonn
Identification of a promising drug candidate for the treatment of type 2 diabetes based on a P2Y(1) receptor agonist.
Bar-Ilan University
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
Structure-activity relationships and optimization of 3,5-dichloropyridine derivatives as novel P2X(7) receptor antagonists.
Gwangju Institute of Science and Technology (Gist)
Discovery of potent competitive antagonists and positive modulators of the P2X2 receptor.
University of Bonn
Benzofuran-substituted urea derivatives as novel P2Y(1) receptor antagonists.
Glaxosmithkline
Identification of hydrolytically stable and selective P2Y(1) receptor agonists.
Bar-Ilan University
Synthesis and in vitro activity of N'-cyano-4-(2-phenylacetyl)-N-o-tolylpiperazine-1-carboximidamide P2X7 antagonists.
Abbott Bioresearch Center
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
Diadenosine and diuridine poly(borano)phosphate analogues: synthesis, chemical and enzymatic stability, and activity at P2Y1 and P2Y2 receptors.
Bar-Ilan University
2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
Universit£
Architecture of P2Y nucleotide receptors: structural comparison based on sequence analysis, mutagenesis, and homology modeling.
National Institute of Diabetes and Digestive and Kidney Diseases
Molecular recognition in purinergic receptors. 2. Diastereoselectivity of the h-P2Y1-receptor.
Bar-Ilan University
Novel antagonists acting at the P2Y(1) purinergic receptor: synthesis and conformational analysis using potentiometric and nuclear magnetic resonance titration techniques.
Universit£
Adenosine 5'-O-(1-boranotriphosphate) derivatives as novel P2Y(1) receptor agonists.
Bar-Ilan University
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
Hit-to-Lead studies: the discovery of potent adamantane amide P2X7 receptor antagonists.
Astrazeneca R&D Charnwood
Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 2.
Merck Research Laboratories
Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X7 receptor.
Pfizer
Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain.
Amgen
Synthesis and biological activity of a series of tetrasubstituted-imidazoles as P2X(7) antagonists.
Glaxosmithkline
Diadenosine 5',5''-(boranated)polyphosphonate analogues as selective nucleotide pyrophosphatase/phosphodiesterase inhibitors.
Bar-Ilan University
Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: part 1.
Merck Research Laboratories
Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X7 receptor antagonists leading to the discovery of the clinical candidate CE-224,535.
Pfizer
Frontal affinity chromatography-mass spectrometry useful for characterization of new ligands for GPR17 receptor.
University of Pavia
Discovery of 2-chloro-N-((4,4-difluoro-1-hydroxycyclohexyl)methyl)-5-(5-fluoropyrimidin-2-yl)benzamide as a potent and CNS penetrable P2X7 receptor antagonist.
Pfizer
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
Synthesis and structure-activity relationships of pyrazolodiazepine derivatives as human P2X7 receptor antagonists.
Institute of Science & Technology
Purinergic P2X(7) receptor antagonists: Chemistry and fundamentals of biological screening.
University of Sydney
Identification and SAR of novel diaminopyrimidines. Part 1: The discovery of RO-4, a dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
Roche Palo Alto
Identification and SAR of novel diaminopyrimidines. Part 2: The discovery of RO-51, a potent and selective, dual P2X(3)/P2X(2/3) antagonist for the treatment of pain.
Roche Palo Alto
Synthesis and structure-activity relationships of novel, substituted 5,6-dihydrodibenzo[a,g]quinolizinium P2X7 antagonists.
Institute of Science and Technology (Gist)
Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists.
Glaxosmithkline
Synthesis and activity of N-cyanoguanidine-piperazine P2X7 antagonists.
Abbott Bioresearch Center
Synthesis and structure-activity relationship studies of tyrosine-based antagonists at the human P2X7 receptor.
Institute of Science and Technology
Discovery of potent and selective adamantane-based small-molecule P2X(7) receptor antagonists/interleukin-1beta inhibitors.
Astrazeneca R&D Charnwood
From tyrosine to glycine: synthesis and biological activity of potent antagonists of the purinergic P2X7 receptor.
Università
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
Drug-like Antagonists of P2Y Receptors-From Lead Identification to Drug Development.
University of Nottingham
Expanding the repertoire of methanocarba nucleosides from purinergic signaling to diverse targets.
National Institute of Diabetes & Digestive & Kidney Diseases
Exploratory study of oxatomide derivatives with high P2X
Takasaki University of Health and Welfare
The Repertoire of Small-Molecule PET Probes for Neuroinflammation Imaging: Challenges and Opportunities beyond TSPO.
Massachusetts General Hospital
Therapeutic potentials and structure-activity relationship of 1,3-benzodioxole N-carbamothioyl carboxamide derivatives as selective and potent antagonists of P2X4 and P2X7 receptors.
Comsats University Islamabad
Design and synthesis of adamantane-1-carbonyl thiourea derivatives as potent and selective inhibitors of h-P2X4 and h-P2X7 receptors: An Emerging therapeutic tool for treatment of inflammation and neurological disorders.
Comsats University Islamabad
Progress of thrombus formation and research on the structure-activity relationship for antithrombotic drugs.
Northwest University
Discovery and synthesis of a novel and selective drug-like P2X(1) antagonist.
Roche Palo Alto
Unveiling the Structure-Activity Relationships at the Orthosteric Binding Site of P2X Ion Channels: The Route to Selectivity.
European Institute For Molecular Imaging (Eimi)
Discovery of Potent Cholinesterase Inhibition-Based Multi-Target-Directed Lead Compounds for Synaptoprotection in Alzheimer's Disease.
Yeditepe University
Structure-Activity Relationship and Neuroprotective Activity of 1,5-Dihydro-2
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and Characterization of the Novel Rodent-Active and CNS-Penetrant P2X7 Receptor Antagonist Lu AF27139.
Lundbeck Research Usa
Discovery of bilirubin as novel P2X7R antagonist with anti-tumor activity.
Zhengzhou University
Synthesis, radiolabeling, and preliminary biological evaluation of [3H]-1-[(S)-N,O-bis-(isoquinolinesulfonyl)-N-methyl-tyrosyl]-4-(o-tolyl)-piperazine, a potent antagonist radioligand for the P2X7 receptor.
Università
Piperazine squaric acid diamides, a novel class of allosteric P2X7 receptor antagonists.
European Institute For Molecular Imaging (Eimi)
Discovery of clinical candidate Sivopixant (S-600918): Lead optimization of dioxotriazine derivatives as selective P2X3 receptor antagonists.
Shionogi
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
Synthesis and biological activity of N-arylpiperazine-modified analogues of KN-62, a potent antagonist of the purinergic P2X7 receptor.
Università
Synthesis and Pharmacological Evaluation of Novel Non-nucleotide Purine Derivatives as P2X7 Antagonists for the Treatment of Neuroinflammation.
Universidad Aut£Noma De Madrid
Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
Pyroglutamide-Based P2X7 Receptor Antagonists Targeting Inflammatory Bowel Disease.
Universit£
Discovery and Structure Relationships of Salicylanilide Derivatives as Potent, Non-acidic P2X1 Receptor Antagonists.
University of Bonn
Potent Suppressive Effects of 1-Piperidinylimidazole Based Novel P2X7 Receptor Antagonists on Cancer Cell Migration and Invasion.
Gwangju Institute of Science and Technology (Gist)
The evolution of P2X7 antagonists with a focus on CNS indications.
Janssen Pharmaceutical Research & Development
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
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists Part 2: Discovery of orally bioavailable compounds.
Shionogi
Synthesis of conformationally constrained analogues of KN62, a potent antagonist of the P2X7-receptor.
Università
Development of High-Throughput Fluorescent-Based Screens to Accelerate Discovery of P2X Inhibitors from Animal Venoms.
University of East Anglia
8-Hydroxy-2-(1H-1,2,3-triazol-1-yl)-1,4-naphtoquinone derivatives inhibited P2X7 Receptor-Induced dye uptake into murine Macrophages.
Fluminense Federal University
A pyridoxine cyclic phosphate and its 6-azoaryl derivative selectively potentiate and antagonize activation of P2X1 receptors.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis and SAR development of quinoline analogs as novel P2X7 receptor antagonists.
Emd Serono Research and Development Institute
Synthesis and in vitro biological evaluation of new P2X7R radioligands [
Indiana University School of Medicine
Antibacterial activity of 2-amino-4-hydroxypyrimidine-5-carboxylates and binding to Burkholderia pseudomallei 2-C-methyl-d-erythritol-2,4-cyclodiphosphate synthase.
Northern Illinois University
New highly active antiplatelet agents with dual specificity for platelet P2Y1 and P2Y12 adenosine diphosphate receptors.
Glsynthesis
Structure-activity relationship studies of pyrimidine-2,4-dione derivatives as potent P2X7 receptor antagonists.
Gwangju Institute of Science and Technology (Gist)
Purinergic receptor P2X?: a novel target for anti-inflammatory therapy.
Punjabi University
New iantherans from the marine sponge Ianthella quadrangulata: novel agonists of the P2Y(11) receptor.
University of Bonn
Recent advances in urea- and thiourea-containing compounds: focus on innovative approaches in medicinal chemistry and organic synthesis.
University of Perugia Via Del Liceo
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
Synthesis and structure-activity relationships of quinolinone and quinoline-based P2X7 receptor antagonists and their anti-sphere formation activities in glioblastoma cells.
Gwangju Institute of Science and Technology (Gist)
1-Aryl-1H- and 2-aryl-2H-1,2,3-triazole derivatives blockade P2X7 receptor in vitro and inflammatory response in vivo.
Instituto De Tecnologia Em F£Rmacos
Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-? Inhibitors.
Pharmaron-Beijing
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 1: Initial structure-activity relationship studies of a hit from a high throughput screening.
Shionogi
4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate.
Janssen Research and Development
A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.
Janssen Research and Development
Pharmacological evaluation of a novel series of urea, thiourea and guanidine derivatives as P2X
The University of Sydney
Discovery of novel purine-based heterocyclic P2X7 receptor antagonists.
Gwangju Institute of Science and Technology
SR147778 [5-(4-bromophenyl)-1-(2,4-dichlorophenyl)-4-ethyl-N-(1-piperidinyl)-1H-pyrazole-3-carboxamide], a new potent and selective antagonist of the CB1 cannabinoid receptor: biochemical and pharmacological characterization.
Sanofi-Synthelabo Recherche
Agonists and antagonists acting at P2X receptors: selectivity profiles and functional implications.
Biocentre Niederursel
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.
Sanofi Recherche