434 articles for thisTarget
The following articles (labelled with PubMed ID or TBD) are for your review
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Article Title
Organization
The 1,2,4-Triazolo[4,3-a]pyrazin-3-one as a Versatile Scaffold for the Design of Potent Adenosine Human Receptor Antagonists. Structural Investigations to Target the A
Universit£
Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A
Advinus Therapeutics
Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A
Advinus Therapeutics
Design, Synthesis, and Pharmacological Characterization of 2-(2-Furanyl)thiazolo[5,4-d]pyrimidine-5,7-diamine Derivatives: New Highly Potent A
Universit£
Synthesis and evaluation of N-substituted 2-amino-4,5-diarylpyrimidines as selective adenosine A
Leiden University
Structure-anticonvulsant activity studies in the group of (E)-N-cinnamoyl aminoalkanols derivatives monosubstituted in phenyl ring with 4-Cl, 4-CH
Jagiellonian University Medical College
Biphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure-Activity Relationships.
RhôNe-Poulenc Rorer
Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT
National Institute Of Diabetes And Digestive And Kidney Diseases
Discovery of 7-(Prolinol-N-yl)-2-phenylamino-thiazolo[5,4-d]pyrimidines as Novel Non-Nucleoside Partial Agonists for the A2A Adenosine Receptor: Prediction from Molecular Modeling.
Julius-Maximilians-Universit£T W£Rzburg
Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine receptors.
Jagiellonian University Medical College
Exploring the 2- and 5-positions of the pyrazolo[4,3-d]pyrimidin-7-amino scaffold to target human A1 and A2A adenosine receptors.
Universit£
Purine (N)-Methanocarba Nucleoside Derivatives Lacking an Exocyclic Amine as Selective A3 Adenosine Receptor Agonists.
National Institute Of Diabetes And Digestive And Kidney Diseases
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes.
Uppsala University
Design, physico-chemical properties and biological evaluation of some new N-[(phenoxy)alkyl]- and N-{2-[2-(phenoxy)ethoxy]ethyl}aminoalkanols as anticonvulsant agents.
Jagiellonian University Medical College
Tetrahydroisoquinoline Phenols: Selective Estrogen Receptor Downregulator Antagonists with Oral Bioavailability in Rat.
Astrazeneca
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity.
University Of Warwick
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions.
Georgia Institute Of Technology
Discovery of aminoquinazoline derivatives as human A(2A) adenosine receptor antagonists.
Merck Research Laboratories
Structural refinement of pyrazolo[4,3-d]pyrimidine derivatives to obtain highly potent and selective antagonists for the human A3 adenosine receptor.
Universit£
5,7-Disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazines as pharmacological tools to explore the antagonist selectivity profiles toward adenosine receptors.
Universit£
Structure-kinetics relationships of Capadenoson derivatives as adenosine A1 receptor agonists.
Leiden University
Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy.
National Institute Of Diabetes And Digestive And Kidney Diseases
Use of molecular modeling aided design to dial out hERG liability in adenosine A(2A) receptor antagonists.
Merck Research Laboratories
One-pot reaction to obtain N,N'-disubstituted guanidines of pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine scaffold as human A3 adenosine receptor antagonists.
Universit£
A solid-phase combinatorial approach for indoloquinolizidine-peptides with high affinity at D(1) and D(2) dopamine receptors.
University Of Barcelona
Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phenylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and selective agonists of the A2A adenosine receptor.
Universit£
5'-C-Ethyl-tetrazolyl-N(6)-substituted adenosine and 2-chloro-adenosine derivatives as highly potent dual acting A1 adenosine receptor agonists and A3 adenosine receptor antagonists.
University Of Camerino
A facile and novel synthesis of N(2)-, C(6)-substituted pyrazolo[3,4-d]pyrimidine-4 carboxylate derivatives as adenosine receptor antagonists.
National University Of Singapore
Synthesis and SAR studies of analogues of 4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-N-thiazol-2-yl-benzamide (Lu AA41063) as adenosine A2A receptor ligands with improved aqueous solubility.
H. Lundbeck
Novel thiazole-thiophene conjugates as adenosine receptor antagonists: synthesis, biological evaluation and docking studies.
B. V. Patel Pharmaceutical Education And Research Development (Perd) Centre
7-Amino-2-phenylpyrazolo[4,3-d]pyrimidine derivatives: structural investigations at the 5-position to target human A1 and A(2A) adenosine receptors. Molecular modeling and pharmacological studies.
Universit£
Scaffold decoration at positions 5 and 8 of 1,2,4-triazolo[1,5-c]pyrimidines to explore the antagonist profiling on adenosine receptors: a preliminary structure-activity relationship study.
Universit£
Extended N(6) substitution of rigid C2-arylethynyl nucleosides for exploring the role of extracellular loops in ligand recognition at the A3 adenosine receptor.
National Institute Of Diabetes And Digestive And Kidney Diseases
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain.
University Of Missouri
1,2,4-triazolo[1,5-a]quinoxaline derivatives and their simplified analogues as adenosine A3 receptor antagonists. Synthesis, structure-affinity relationships and molecular modeling studies.
Universit£
Further studies on pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as potent and selective human A1 adenosine receptor antagonists.
Universit£
Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis and biological evaluation of novel allosteric enhancers of the A1 adenosine receptor based on 2-amino-3-(4'-chlorobenzoyl)-4-substituted-5-arylethynyl thiophene.
Universit£
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
Astrazeneca
Agonists for the adenosine A1 receptor with tunable residence time. A Case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines.
Leiden University
Structure-based approaches to ligands for G-protein-coupled adenosine and P2Y receptors, from small molecules to nanoconjugates.
National Institute Of Diabetes And Digestive And Kidney Diseases
Substituted 7-amino-5-thio-thiazolo[4,5-d]pyrimidines as potent and selective antagonists of the fractalkine receptor (CX3CR1).
Astrazeneca
2-Arylpyrazolo[4,3-d]pyrimidin-7-amino derivatives as new potent and selective human A3 adenosine receptor antagonists. Molecular modeling studies and pharmacological evaluation.
Universit£
Synthesis and structure-activity relationships of 2-hydrazinyladenosine derivatives as A(2A) adenosine receptor ligands.
University Of Bonn
Selective and potent adenosine A3 receptor antagonists by methoxyaryl substitution on the N-(2,6-diarylpyrimidin-4-yl)acetamide scaffold.
University Of Santiago De Compostela
Pyrazolo[1,5-c]quinazoline derivatives and their simplified analogues as adenosine receptor antagonists: synthesis, structure-affinity relationships and molecular modeling studies.
Universita' Di Firenze
Highly potent and selective fluorescent antagonists of the human adenosine A3 receptor based on the 1,2,4-triazolo[4,3-a]quinoxalin-1-one scaffold.
University Of Nottingham
New fluorescent adenosine A1-receptor agonists that allow quantification of ligand-receptor interactions in microdomains of single living cells.
University Of Nottingham
Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions.
TBA
Synthesis and pharmacological evaluation of novel substituted 9-deazaxanthines as A2B receptor antagonists.
Universidade De A Coru£A
In silico directed chemical probing of the adenosine receptor family.
Universidade Do Minho
Synthesis and pharmacological evaluation of novel 1,3,8- and 1,3,7,8-substituted xanthines as adenosine receptor antagonists.
Universidade De Porto
Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor.
Universit£
Exploring the directionality of 5-substitutions in a new series of 5-alkylaminopyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine as a strategy to design novel human a(3) adenosine receptor antagonists.
Universit£
Medicinal chemistry of A3 adenosine receptor modulators: pharmacological activities and therapeutic implications.
Universit£
Structural sweet spot for A1 adenosine receptor activation by truncated (N)-methanocarba nucleosides: receptor docking and potent anticonvulsant activity.
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[(4-arylpiperazin-1-yl)methyl]-5-substituted-thiophenes. effect of the 5-modification on allosteric enhancer activity at the A1 adenosine receptor.
Universit£
Identifying novel adenosine receptor ligands by simultaneous proteochemometric modeling of rat and human bioactivity data.
Leiden/Amsterdam Center For Drug Research
Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice.
University Of North Carolina At Chapel Hill
Design and characterization of optimized adenosine A2A/A1 receptor antagonists for the treatment of Parkinson's disease.
Janssen Research And Development
Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones.
Jagiellonian University Medical College
Structure-activity relationships and molecular modeling of 1,2,4-triazoles as adenosine receptor antagonists.
TBA
Water-soluble pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines as human A3 adenosine receptor antagonists.
Universit£
Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.
National Institute Of Diabetes And Digestive And Kidney Diseases
Structure-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.
National Institute Of Diabetes And Digestive And Kidney Diseases
New chromene scaffolds for adenosine A(2A) receptors: synthesis, pharmacology and structure-activity relationships.
Universidade Do Minho
Synthesis and pharmacological evaluation of dual acting antioxidant A(2A) adenosine receptor agonists.
Monash University
Development of Polar Adenosine A2A Receptor Agonists for Inflammatory Bowel Disease: Synergism with A2B Antagonists.
TBA
Exploring activity cliffs in medicinal chemistry.
Rheinische Friedrich-Wilhelms-Universit£T
3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A2B adenosine receptor antagonists.
Universit£
Discovery of 1,2,4-triazine derivatives as adenosine A(2A) antagonists using structure based drug design.
Heptares Therapeutics
Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.
TBA
Discovery of phosphoric acid mono-{2-[(E/Z)-4-(3,3-dimethyl-butyrylamino)-3,5-difluoro-benzoylimino]-thiazol-3-ylmethyl} ester (Lu AA47070): a phosphonooxymethylene prodrug of a potent and selective hA(2A) receptor antagonist.
H. Lundbeck
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela
Pfizer
Discovery of a novel 5-HT(3) antagonist/5-HT(1A) agonist 3-amino-5,6,7,8-tetrahydro-2-{4-[4-(quinolin-2-yl)piperazin-1-yl]butyl}quinazolin-4(3H)-one (TZB-30878) as an orally bioavailable agent for irritable bowel syndrome.
Aska Pharmaceutical
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists.
Roche Research Center
Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation.
Universit£
Novel 8-(furan-2-yl)-3-substituted thiazolo [5,4-e][1,2,4] triazolo[1,5-c] pyrimidine-2(3H)-thione derivatives as potential adenosine A(2A) receptor antagonists.
University Of Delhi
2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists.
University Of Bonn
1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity.
Institute
High-affinity, non-nucleotide-derived competitive antagonists of platelet P2Y12 receptors.
University Of Bonn
8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands.
University Of Camerino
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists.
Leiden/Amsterdam Center For Drug Research
Luteolin, a compound with adenosine A(1) receptor-binding activity, and chromone and dihydronaphthalenone constituents from Senna siamea.
Leiden University
Alkaloids from Eschscholzia californica and their capacity to inhibit binding of [3H]8-Hydroxy-2-(di-N-propylamino)tetralin to 5-HT1A receptors in Vitro.
Tom'S Of Maine
Synthesis of eudistomin D analogues and its effects on adenosine receptors.
Hokkaido University
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.
National Institute Of Diabetes And Digestive And Kidney Diseases
Antagonists of the human adenosine A2A receptor. Part 3: Design and synthesis of pyrazolo[3,4-d]pyrimidines, pyrrolo[2,3-d]pyrimidines and 6-arylpurines.
Vernalis (R&D)
Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives.
Vernalis (R&D)
Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives.
Vernalis (R&D)
Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases.
Cv Therapeutics
Probing distal regions of the A2B adenosine receptor by quantitative structure-activity relationship modeling of known and novel agonists.
National Institute Of Diabetes And Digestive And Kidney Diseases
1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A(2B) adenosine receptor antagonists.
Universit£
N6-substituted C5'-modified adenosines as A1 adenosine receptor agonists.
Monash University (Parkville Campus)
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines.
Leiden/Amsterdam Center For Drug Research
1-, 3- and 8-substituted-9-deazaxanthines as potent and selective antagonists at the human A2B adenosine receptor.
Universit£
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat.
Abbott Laboratories
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists.
Ewha Womans University
5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.
Universit£
Potent and selective xanthine-based inhibitors of phosphodiesterase 5.
Novartis Institutes Of Biomedical Research
Structure-activity relationships of adenosines with heterocyclic N6-substituents.
Monash University (Parkville Campus)
5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.
Universit£
N(6)-[(hetero)aryl/(cyclo)alkyl-carbamoyl-methoxy-phenyl]-(2-chloro)-5'-N-ethylcarboxamido-adenosines: the first example of adenosine-related structures with potent agonist activity at the human A(2B) adenosine receptor.
Universit£
Structure-activity relationships of 2,N(6),5'-substituted adenosine derivatives with potent activity at the A2B adenosine receptor.
National Institute Of Diabetes And Digestive And Kidney Diseases
N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor.
Universit£
Synthesis and biological evaluation of novel 1-deoxy-1-[6-[((hetero)arylcarbonyl)hydrazino]- 9H-purin-9-yl]-N-ethyl-beta-D-ribofuranuronamide derivatives as useful templates for the development of A2B adenosine receptor agonists.
Universit£
SAR of a series of 5,6-dihydro-(9H)-pyrazolo[3,4-c]-1,2,4-triazolo[4,3-alpha]pyridines as potent inhibitors of human eosinophil phosphodiesterase.
Pfizer
Structure-activity relationship study of prion inhibition by 2-aminopyridine-3,5-dicarbonitrile-based compounds: parallel synthesis, bioactivity, and in vitro pharmacokinetics.
University Of California San Francisco
N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.
University Of Virginia
Synthesis and biological studies of a new series of 5-heteroarylcarbamoylaminopyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidines as human A3 adenosine receptor antagonists. Influence of the heteroaryl substituent on binding affinity and molecular modeling investigations.
Universit£
2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching.
Universit£
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£
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.
Leiden/Amsterdam Center For Drug Research
Binding thermodynamics as a tool to investigate the mechanisms of drug-receptor interactions: thermodynamics of cytoplasmic steroid/nuclear receptors in comparison with membrane receptors.
University Of Ferrara
Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.
Universit£
6-aryl-8H-indeno[1,2-d]thiazol-2-ylamines: A1 adenosine receptor agonist allosteric enhancers having improved potency.
University Of Virginia
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.
Universit£
2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists.
Cv Therapeutics
Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor.
Iiqab (Csic)
A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential.
Novartis Institutes For Biomedical Research
Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor.
Ewha Womans University
Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists.
Universit£
New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine.
University Of Leiden
1,2,4-triazolo[4,3-a]quinoxalin-1-one moiety as an attractive scaffold to develop new potent and selective human A3 adenosine receptor antagonists: synthesis, pharmacological, and ligand-receptor modeling studies.
Universit£
Incorporating molecular shape into the alignment-free Grid-Independent Descriptors.
Universitat Pompeu Fabra
N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor.
Leiden University
Design, synthesis, and biological evaluation of C9- and C2-substituted pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as new A2A and A3 adenosine receptors antagonists.
Universit£
N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands.
Universit£
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.
National Institute Of Diabetes
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.
Leiden University
Adenosine A1 antagonists. 3. Structure-activity relationships on amelioration against scopolamine- or N6-((R)-phenylisopropyl)adenosine-induced cognitive disturbance.
Kyowa Hakko Kogyo
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Virginia Commonwealth University
7-Nitrobenzofurazan (NBD) derivatives of 5'-N-ethylcarboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors.
Universit£
Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor.
Universit£
Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications.
Niddk
Diimidazo[1,2-c:4',5'-e]pyrimidines: adenosine agonist activity demonstrated by microphysiometry.
Griffith University
New base-altered adenosine analogues: Synthesis and affinity at adenosine A1 and A2A receptors
TBA
Novel 1,3-dipropyl-8-(3-benzimidazol-2-yl-methoxy-1-methylpyrazol-5-yl)xanthines as potent and selective A2B adenosine receptor antagonists.
University Of Ferrara
Evaluation of molecular modeling of agonist binding in light of the crystallographic structure of an agonist-bound A2A adenosine receptor.
National Institute Of Diabetes And Digestive And Kidney Diseases
Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A2A and A3 adenosine receptor ligands.
Ewha Womans University
Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists.
Universit£
Synthesis and Biological Evaluation of a New Series of 1,2,4-Triazolo[1,5-a]-1,3,5-triazines as Human A(2A) Adenosine Receptor Antagonists with Improved Water Solubility.
Universita Di Trieste
Investigation of the pyrazinones as PDE5 inhibitors: evaluation of regioisomeric projections into the solvent region.
Pfizer
Does the combination of optimal substitutions at the C²-, N¿?¿- and N¿?¿-positions of the pyrazolo-triazolo-pyrimidine scaffold guarantee selective modulation of the human A3 adenosine receptors?
National University Of Singapore
New 2-heterocyclyl-imidazo[2,1-i]purin-5-one derivatives as potent and selective human A3 adenosine receptor antagonists.
Universit£
Synthesis, structure-affinity relationships, and molecular modeling studies of novel pyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.
Universita' Di Firenze
Molecular probes for the A2A adenosine receptor based on a pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine scaffold.
National Institute Of Diabetes And Digestive And Kidney Diseases
Discovery of benzothiazole-based adenosine A2B receptor antagonists with improved A2A selectivity.
Roche Research Center
Design and optimisation of orally active TLR7 agonists for the treatment of hepatitis C virus infection.
Pfizer
Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist
TBA
Pyrimidine derivatives as potent and selective A3 adenosine receptor antagonists.
University Of Santiago De Compostela
In vivo characterization of a dual adenosine A2A/A1 receptor antagonist in animal models of Parkinson's disease.
Johnson & Johnson Pharmaceutical Research And Development
Molecular modeling study on potent and selective adenosine A(3) receptor agonists.
University Of Camerino
Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands.
Dipartimento Di Scienze Farmaceutiche
Identification and optimization of substituted 5-aminopyrazoles as potent and selective adenosine A1 receptor antagonists.
Bayer Schering Pharma
Design, synthesis, and binding of homologated truncated 4'-thioadenosine derivatives at the human A3 adenosine receptors.
Ewha Womans University
Hit-to-lead optimization of a series of carboxamides of ethyl 2-amino-4-phenylthiazole-5-carboxylates as novel adenosine A2A receptor antagonists.
H. Lundbeck
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase.
Università
Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods.
East China University Of Science And Technology
Synthesis and evaluation of new N6-substituted adenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists.
Monash University
Methylene amine substituted arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.
Johnson & Johnson Pharmaceutical Research And Development
Optimization of arylindenopyrimidines as potent adenosine A(2A)/A(1) antagonists.
Johnson & Johnson Pharmaceutical Research And Development
The significance of 2-furyl ring substitution with a 2-(para-substituted) aryl group in a new series of pyrazolo-triazolo-pyrimidines as potent and highly selective hA(3) adenosine receptors antagonists: new insights into structure-affinity relationship and receptor-antagonist recognition.
National University Of Singapore
Discovery of potent and selective bicyclic A(2B) adenosine receptor antagonists via bioisosteric amide replacement.
RhôNe-Poulenc Rorer
Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists.
RhôNe-Poulenc Rorer
Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists.
Novartis Institutes For Biomedical Research
Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors.
Universidad De M£Laga
Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists.
Ewha Womans University
3- and 6-Substituted 2-amino-4,5,6,7-tetrahydrothieno[2,3-c]pyridines as A1 adenosine receptor allosteric modulators and antagonists.
Monash University (Parkville Campus)
2-Phenylpyrazolo[4,3-d]pyrimidin-7-one as a new scaffold to obtain potent and selective human A3 adenosine receptor antagonists: new insights into the receptor-antagonist recognition.
Universit£
Functionalized congeners of A3 adenosine receptor-selective nucleosides containing a bicyclo[3.1.0]hexane ring system.
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis and biological evaluation of 2-alkynyl-N6-methyl-5'-N-methylcarboxamidoadenosine derivatives as potent and highly selective agonists for the human adenosine A3 receptor.
University Of Camerino
Design, synthesis and biological evaluation of a bivalent micro opiate and adenosine A1 receptor antagonist.
Aix-Marseille Universit£
Combining selectivity and affinity predictions using an integrated Support Vector Machine (SVM) approach: An alternative tool to discriminate between the human adenosine A(2A) and A(3) receptor pyrazolo-triazolo-pyrimidine antagonists binding sites.
Universit£
Synthesis of hybrid analogues of caffeine and eudistomin D and its affinity for adenosine receptors.
Hokkaido University
Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.
Ewha Womans University
Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides.
Vernalis (R+D)
The discovery of CP-96,021 and CP-96,486, balanced, combined, potent and orally active leukotriene D4 (LTD4)/platelet activating factor (PAF) receptor antagonists.
TBA
1,3-dialkyl-8-N-substituted benzyloxycarbonylamino-9-deazaxanthines as potent adenosine receptor ligands: Design, synthesis, structure-affinity and structure-selectivity relationships.
Universidade De Santiago De Compostela
N6-Cycloalkyl- and N6-bicycloalkyl-C5'(C2')-modified adenosine derivatives as high-affinity and selective agonists at the human A1 adenosine receptor with antinociceptive effects in mice.
University Of Camerino
Pyrido[2,3-e]-1,2,4-triazolo[4,3-a]pyrazin-1-one as a new scaffold to develop potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
Universita Di Firenze
Synthesis and SAR studies of trisubstituted purinones as potent and selective adenosine A2A receptor antagonists.
Pharmacopeia
N-[6-amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A receptor antagonists with improved drug like properties and in vivo efficacy.
Neurocrine Biosciences
Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines.
Vernalis R&D
Synthesis of 2-amino-5-benzoyl-4-(2-furyl)thiazoles as adenosine A(2A) receptor antagonists.
Pharmacopeia
Synthesis of a series of 8-(substituted-phenyl)xanthines and a study on the effects of substitution pattern of phenyl substituents on affinity for adenosine A(1) and A(2A) receptors.
University Institute Of Pharmaceutical Sciences
Structure-activity relationship studies of a new series of imidazo[2,1-f]purinones as potent and selective A(3) adenosine receptor antagonists.
Università
Novel potent and highly selective human A(3) adenosine receptor antagonists belonging to the 4-amido-2-arylpyrazolo[3,4-c]quinoline series: molecular docking analysis and pharmacological studies.
Università
1,3-Dialkyl-8-(hetero)aryl-9-OH-9-deazaxanthines as potent A2B adenosine receptor antagonists: design, synthesis, structure-affinity and structure-selectivity relationships.
Università
2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability.
Neurocrine Biosciences
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.
Ewha Womans University
2-aminothienopyridazines as novel adenosine A1 receptor allosteric modulators and antagonists.
Monash University
Selective A(3) adenosine receptor antagonists derived from nucleosides containing a bicyclo[3.1.0]hexane ring system.
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis and biological evaluation of 2-amino-3-(4-chlorobenzoyl)-4-[N-(substituted) piperazin-1-yl]thiophenes as potent allosteric enhancers of the A1 adenosine receptor.
Dipartimento Di Scienze Farmaceutiche
Synthesis, ligand-receptor modeling studies and pharmacological evaluation of novel 4-modified-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives as potent and selective human A3 adenosine receptor antagonists.
Universita' Di Firenze
Lignans isolated from valerian: identification and characterization of a new olivil derivative with partial agonistic activity at A(1) adenosine receptors.
University Of Bonn
Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.
Neurocrine Biosciences
Selective, high affinity A(2B) adenosine receptor antagonists: N-1 monosubstituted 8-(pyrazol-4-yl)xanthines.
Cv Therapeutics
Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy.
Neurocrine Biosciences
Phenylethyl-substituted pyrimido[2,1-f]purinediones and related compounds: structure-activity relationships as adenosine A(1) and A(2A) receptor ligands.
Jagiellonian University Medical College
Dual acting antioxidant A1 adenosine receptor agonists.
Monash University (Parkville Campus)
New 2-arylpyrazolo[3,4-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. Synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
Università
Design, synthesis, and biological evaluation of LNA nucleosides as adenosine A3 receptor ligands.
Santaris Pharma
Discovery of a new nucleoside template for human A3 adenosine receptor ligands: D-4'-thioadenosine derivatives without 4'-hydroxymethyl group as highly potent and selective antagonists.
Ewha Womans University
Novel ergopeptides as dual ligands for adenosine and dopamine receptors.
Institut D'Investigacions BiomèDiques August Pi I
N9-benzyl-substituted 1,3-dimethyl- and 1,3-dipropyl-pyrimido[2,1-f]purinediones: synthesis and structure-activity relationships at adenosine A1 and A2A receptors.
Jagiellonian University
Discovery and characterization of 4'-(2-furyl)-N-pyridin-3-yl-4,5'-bipyrimidin-2'-amine (LAS38096), a potent, selective, and efficacious A2B adenosine receptor antagonist.
Almirall
2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists.
Leiden/Amsterdam Center For Drug Research
Potent, selective, and orally active adenosine A2A receptor antagonists: arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines.
Schering-Plough Research Institute
2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists.
Ghent University
Tricyclic imidazoline derivatives as potent and selective adenosine A1 receptor antagonists.
Biogen Idec
Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists.
Biogen Idec
N6-Cycloalkyl-2-substituted adenosine derivatives as selective, high affinity adenosine A1 receptor agonists.
Cv Therapeutics
Identification of non-furan containing A2A antagonists using database mining and molecular similarity approaches.
Vernalis (R&D)
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists.
University Of Bonn
Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models.
Università
4-amido-2-aryl-1,2,4-triazolo[4,3-a]quinoxalin-1-ones as new potent and selective human A3 adenosine receptor antagonists. synthesis, pharmacological evaluation, and ligand-receptor modeling studies.
Università
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists.
Cv Therapeutics
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
Leiden University
New pyrrolopyrimidin-6-yl benzenesulfonamides: potent A2B adenosine receptor antagonists.
RhôNe-Poulenc Rorer
2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists.
Leiden/Amsterdam Center For Drug Research
Synthesis, in vitro and in vivo evaluation of [O-methyl-11C] 2-{4-[4-(3-methoxyphenyl)piperazin-1-yl]-butyl}-4-methyl-2H-[1,2,4]-triazine-3,5-dione: a novel agonist 5-HT1A receptor PET ligand.
Columbia University College Of Physicians And Surgeons
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-uronamides as highly potent and selective agonists at the human A3 adenosine receptor.
Ewha Womans University
Semi-rational design of (north)-methanocarba nucleosides as dual acting A(1) and A(3) adenosine receptor agonists: novel prototypes for cardioprotection.
National Institute Of Diabetes And Digestive And Kidney Diseases
1,2,4-Triazolo[1,5-a]quinoxaline as a versatile tool for the design of selective human A3 adenosine receptor antagonists: synthesis, biological evaluation, and molecular modeling studies of 2-(hetero)aryl- and 2-carboxy-substituted derivatives.
Università
Synthesis and biological characterization of [3H] (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)-methanone, the first radiolabelled adenosine A1 allosteric enhancer.
Università
Conversion of A3 adenosine receptor agonists into selective antagonists by modification of the 5'-ribofuran-uronamide moiety.
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis and 3D QSAR of new pyrazolo[3,4-b]pyridines: potent and selective inhibitors of A1 adenosine receptors.
Università
Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists.
Cv Therapeutics
1,8-Naphthyridin-4-one derivatives as new ligands of A2A adenosine receptors.
Dipartimento Di Scienze Farmaceutiche
New 2-arylpyrazolo[4,3-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists.
Università
"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists.
National Institute Of Diabetes And Digestive And Kidney Diseases
New pyrrolo[2,1-f]purine-2,4-dione and imidazo[2,1-f]purine-2,4-dione derivatives as potent and selective human A3 adenosine receptor antagonists.
Università
GPCR Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A
University Of Southern California
Surface Plasmon Resonance Screening to Identify Active and Selective Adenosine Receptor Binding Fragments.
University Of Dundee
Discovery of small-molecule compounds and natural products against Parkinson's disease: Pathological mechanism and structural modification.
Zhejiang University
Adenosine receptor antagonists: Recent advances and therapeutic perspective.
Isf College Of Pharmacy
Dual A1/A3 Adenosine Receptor Antagonists: Binding Kinetics and Structure-Activity Relationship Studies Using Mutagenesis and Alchemical Binding Free Energy Calculations.
National And Kapodistrian University Of Athens
(N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists.
National Institute Of Diabetes And Digestive And Kidney Diseases
The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.
Cv Therapeutics
Discovery and Structure-Activity Relationship Studies of Novel Adenosine A
University Of Bern
2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists.
Leiden/Amsterdam Center For Drug Research
Optimization of 2-Amino-4,6-diarylpyrimidine-5-carbonitriles as Potent and Selective A
Universidade De Santiago De Compostela
Development and Application of Subtype-Selective Fluorescent Antagonists for the Study of the Human Adenosine A
Monash University
Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists.
Biogen Idec
Crystal Structure and Subsequent Ligand Design of a Nonriboside Partial Agonist Bound to the Adenosine A
Leiden University
Exploring Non-orthosteric Interactions with a Series of Potent and Selective A
Universidade De Santiago De Compostela
Structure-activity relationships of adenosine A3 receptor ligands: new potential therapy for the treatment of glaucoma.
Otsuka Pharmaceutical Factory
A mild, efficient and alpha-selective glycosidation by using potassium dodecatungstocobaltate trihydrate as catalyst.
University Of Isfahan
Structure-Based Design of Dual-Acting Compounds Targeting Adenosine A
Shanghaitech University
Subtle Chemical Changes Cross the Boundary between Agonist and Antagonist: New A
Ewha Womans University
Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.
Università
Comparison of inhibitory activity of isomeric triazolopyridine derivatives towards adenosine receptor subtypes or do similar structures reveal similar bioactivities?
F. Hoffmann-La Roche
JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.
Janssen Research & Development
2-(N-acyl) and 2-N-acyl-N(6)-substituted analogues of adenosine and their affinity at the human adenosine receptors.
Inotek Pharmaceuticals
Synthesis and SAR evaluation of 1,2,4-triazoles as A(2A) receptor antagonists.
F. Hoffmann-La Roche
Synthesis and biological evaluation of 2,3,5-substituted [1,2,4]thiadiazoles as allosteric modulators of adenosine receptors.
Leiden University
Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor--efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF).
Cv Therapeutics
Design, synthesis and biological evaluation of novel scaffold benzo[4,5]imidazo [1,2-a]pyrazin-1-amine: Towards adenosine A
Sun Yat-Sen University
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as adenosine receptor antagonists. Influence of the N5 substituent on the affinity at the human A 3 and A 2B adenosine receptor subtypes: a molecular modeling investigation.
Università
2-Amino-3-benzoylthiophene allosteric enhancers of A1 adenosine agonist binding: new 3, 4-, and 5-modifications.
Deakin University
Design, synthesis and biological evaluation of Tozadenant analogues as adenosine A
University Of Cologne
Direct Comparison of (N)-Methanocarba and Ribose-Containing 2-Arylalkynyladenosine Derivatives as A
National Institute Of Diabetes And Digestive And Kidney Disease
3'-Aminoadenosine-5'-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor.
Pfizer
New irreversible adenosine A(1) antagonists based on FSCPX.
Monash University (Parkville Campus)
Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor.
Cv Therapeutics
1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands.
Nutrition Research Institute
Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A(3) adenosine receptor antagonist.
TBA
Pyrido[2,1-f]purine-2,4-dione derivatives as a novel class of highly potent human A(3) adenosine receptor antagonists.
Instituto De QuíMica MéDica (Csic)
2-Aminothiazoles: a new class of agonist allosteric enhancers of A(1) adenosine receptors.
University Of Virginia
Biological Evaluation of 5'-(
National Institute Of Diabetes And Digestive And Kidney Diseases
5'-Deoxy congeners of 9-(3-amido-3-deoxy-beta-D-xylofuranosyl)-N(6)-cyclopentyladenine: new adenosine A(1) receptor antagonists and inverse agonists.
Ghent University
1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists.
University Of Bonn
Substituted 4-phenylthiazoles: Development of potent and selective A
University Of Bonn
Synthesis, biological activity, and molecular modeling investigation of new pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as human A(3) adenosine receptor antagonists.
Università
7-Substituted 5-amino-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as A2A adenosine receptor antagonists: a study on the importance of modifications at the side chain on the activity and solubility.
Università
Ocular Disease Therapeutics: Design and Delivery of Drugs for Diseases of the Eye.
Taipei Medical University
New 8-amino-1,2,4-triazolo[4,3-a]pyrazin-3-one derivatives. Evaluation of different moieties on the 6-aryl ring to obtain potent and selective human A
Universit£
Structural investigation on thiazolo[5,4-d]pyrimidines to obtain dual-acting blockers of CD73 and adenosine A
Universit£
Fluorosulfonyl- and bis-(beta-chloroethyl)amino-phenylamino functionalized pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives: irreversible antagonists at the human A3 adenosine receptor and molecular modeling studies.
Università
Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent A
Uppsala University
2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic glucose production induced via agonism of the A(2B) receptor.
Eisai
Fluorosulfonyl-substituted xanthines as selective irreversible antagonists for the A(1)-adenosine receptor.
Deakin University
Pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists: influence of the chain at the N(8) pyrazole nitrogen.
Università
Design, radiosynthesis, and biodistribution of a new potent and selective ligand for in vivo imaging of the adenosine A(2A) receptor system using positron emission tomography.
University Of Milano-Bicocca
Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies.
Jagiellonian University Medical College
8-Substituted 1,3-dimethyltetrahydropyrazino[2,1-f]purinediones: Water-soluble adenosine receptor antagonists and monoamine oxidase B inhibitors.
University Of Bonn
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.
National Institute Of Diabetes
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.
Palack£
Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors.
Università
Water-soluble phosphate prodrugs of 1-propargyl-8-styrylxanthine derivatives, A(2A)-selective adenosine receptor antagonists.
University Of WüRzburg
Modifications on the Amino-3,5-dicyanopyridine Core To Obtain Multifaceted Adenosine Receptor Ligands with Antineuropathic Activity.
Universit£
Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A
Medical College Of Wisconsin
Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists.
Università
Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays.
Cadus Pharmaceutical
Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A
Leiden University
Design, synthesis and biological evaluation of 2-hydrazinyladenosine derivatives as A
National Engineering Research Center For The Emergency Drug
Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances.
University Of Science & Technology (Ust)
Design, synthesis, and biological evaluation of a second generation of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidines as potent and selective A2A adenosine receptor antagonists.
Università
Novel human adenosine receptor antagonists based on the 7-amino-thiazolo[5,4-d]pyrimidine scaffold. Structural investigations at the 2-, 5- and 7-positions to enhance affinity and tune selectivity.
Universit£
Synthesis and biological evaluation of the enantiomers of the potent and selective A1-adenosine antagonist 1,3-dipropyl-8-[2-(5,6-epoxynorbonyl)]-xanthine.
Cv Therapeutics
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.
National Institute Of Diabetes
Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models.
Stockholm University
Structure-Based Design, Synthesis by Click Chemistry and
National Institute Of Diabetes And Digestive And Kidney Diseases
Synthesis and anti-renal fibrosis activity of conformationally locked truncated 2-hexynyl-N(6)-substituted-(N)-methanocarba-nucleosides as A3 adenosine receptor antagonists and partial agonists.
Seoul National University
Novel 8-(p-substituted-phenyl/benzyl)xanthines with selectivity for the A2A adenosine receptor possess bronchospasmolytic activity.
Panjab University
Discovery of simplified Nē-substituted pyrazolo[3,4-d]pyrimidine derivatives as novel adenosine receptor antagonists: efficient synthetic approaches, biological evaluations and molecular docking studies.
National University Of Singapore
1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases.
University Of Bonn
Discovery of 3,4-Dihydropyrimidin-2(1H)-ones As a Novel Class of Potent and Selective A2B Adenosine Receptor Antagonists.
University Of Santiago De Compostela
8-(2-Furyl)adenine derivatives as A?A adenosine receptor ligands.
University Of Camerino
Substituted 1,3-dipropylxanthines as irreversible antagonists of A1 adenosine receptors.
University Of South Florida
Design and synthesis of (4E)-4-(4-substitutedbenzylideneamino)-3-substituted-2,3-dihydro-2-thioxothiazole-5-carbonitrile as novel A2A receptor antagonists.
University Of Delhi
Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease.
Universit£
New insight into adenosine receptors selectivity derived from a novel series of [5-substituted-4-phenyl-1,3-thiazol-2-yl] benzamides and furamides.
B.V. Patel Pharmaceutical Education And Research Development
Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones.
University Of Bonn
Novel adenosine A(2A) receptor ligands: a synthetic, functional and computational investigation of selected literature adenosine A(2A) receptor antagonists for extending into extracellular space.
Monash University (Parkville Campus)
Substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists.
Janssen Research & Development
Synthesis, adenosine receptor binding and 3D-QSAR of 4-substituted 2-(2'-furyl)-1,2,4-triazolo[1,5-a]quinoxalines.
University Of Santiago De Compostela
Synthesis and biological evaluation of a new series of 2,3,5-substituted [1,2,4]-thiadiazoles as modulators of adenosine A1 receptors and their molecular mechanism of action.
Leiden/Amsterdam Center For Drug Research
Discovery of 6-oxo-3-(2-phenylpyrazolo[1,5-a]pyridin-3-yl)-1(6H)- pyridazinebutanoic acid (FK 838): a novel non-xanthine adenosine A1 receptor antagonist with potent diuretic activity.
Fujisawa Pharmaceutical
[1,2,4]Triazolo[1,5-c]pyrimidines as adenosine receptor antagonists: Modifications at the 8 position to reach selectivity towards A
Universit£
Antagonists of the adenosine A
Umr-S1172 - Jparc - Centre De Recherche Jean-Pierre Aubert Neurosciences Et Cancer
The aminopyridine-3,5-dicarbonitrile core for the design of new non-nucleoside-like agonists of the human adenosine A
Universit£
Structure-activity relationship studies and pharmacological characterization of N
Universit£
2,4-Diaminoquinazolines as Dual Toll-like Receptor (TLR) 7/8 Modulators for the Treatment of Hepatitis B Virus.
Janssen Infectious Diseases-Diagnostics
Docking Screens for Dual Inhibitors of Disparate Drug Targets for Parkinson's Disease.
Uppsala University
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t.
Phenex Pharmaceuticals
Imidazo[1,2-a]pyrazin-8-amine core for the design of new adenosine receptor antagonists: Structural exploration to target the A
Universita Degli Studi Di Firenze
Structure-activity relationships of 8-cycloalkyl-1,3-dipropylxanthines as antagonists of adenosine receptors.
Vanderbilt University
Structure-Based Design, Synthesis, and In Vivo Antinociceptive Effects of Selective A
University Of Camerino
An allosteric PRC2 inhibitor targeting the H3K27me3 binding pocket of EED.
Novartis Institutes For Biomedical Research
Structure-Based Screening of Uncharted Chemical Space for Atypical Adenosine Receptor Agonists
Uppsala University
4-amino-6-alkyloxy-2-alkylthiopyrimidine derivatives as novel non-nucleoside agonists for the adenosine A1 receptor.
Universit?? Di Napoli Federico Ii
Synthesis and pharmacological characterization of novel xanthine carboxylate amides as A2A adenosine receptor ligands exhibiting bronchospasmolytic activity.
Panjab University
Development of novel adenosine receptor ligands based on the 3-amidocoumarin scaffold.
Universidade Do Porto
Synthesis of hybrid molecules of caffeine and eudistomin D and its effects on adenosine receptors.
Hokkaido University
Desvenlafaxine succinate: A new serotonin and norepinephrine reuptake inhibitor.
Wyeth Research
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
A(3) adenosine receptors in human neutrophils and promyelocytic HL60 cells: a pharmacological and biochemical study.
University Of Ferrara
Extended radioligand binding profile of iloperidone: a broad spectrum dopamine/serotonin/norepinephrine receptor antagonist for the management of psychotic disorders.
Novartis Pharma
Characterization of human A(2B) adenosine receptors: radioligand binding, western blotting, and coupling to G(q) in human embryonic kidney 293 cells and HMC-1 mast cells.
University Of Virginia
2-Substituted N-ethylcarboxamidoadenosine derivatives as high-affinity agonists at human A3 adenosine receptors.
Universitat Wurzburg
Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.
Schering-Plough Research Institute
SR 144528, the first potent and selective antagonist of the CB2 cannabinoid receptor.
Sanofi Recherche
Cloning, expression and pharmacological characterization of rabbit adenosine A1 and A3 receptors.
Pfizer
A-85380 [3-(2(S)-azetidinylmethoxy) pyridine]: in vitro pharmacological properties of a novel, high affinity alpha 4 beta 2 nicotinic acetylcholine receptor ligand.
Abbott Laboratories
(S)-3-methyl-5-(1-methyl-2-pyrrolidinyl) isoxazole (ABT 418): a novel cholinergic ligand with cognition-enhancing and anxiolytic activities: I. In vitro characterization.
Abbott Laboratories
A neoceptor approach to unraveling microscopic interactions between the human A2A adenosine receptor and its agonists.
National Institutes Of Health
Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides.
Vernalis (R&D)
Lead Optimization of 4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A Adenosine Receptor Antagonists for the Treatment of Parkinson's Disease.
Neurocrine Bioscience
Synthesis of bivalent beta2-adrenergic and adenosine A1 receptor ligands.
Monash University
Derivatives of 4-Amino-6-hydroxy-2-mercaptopyrimidine as Novel, Potent, and Selective A3 Adenosine Receptor Antagonists.
Universita Di Napoli
2-Amino-N-pyrimidin-4-ylacetamides as A2A Receptor Antagonists: 2. Reduction of hERG Activity, Observed Species Selectivity, and Structure-Activity Relationships.
Neuroscience