427 articles for thisTarget
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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
Universita Degli Studi Di Firenze
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
Novartis Pharma
Scaffold Repurposing of Nucleosides (Adenosine Receptor Agonists): Enhanced Activity at the Human Dopamine and Norepinephrine Sodium Symporters.
National Institute of Diabetes and Digestive and Kidney Diseases
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
Universita Degli Studi Di Firenze
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
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.
Universita Degli Studi Di Firenze
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
Tactical Approaches to Interconverting GPCR Agonists and Antagonists.
University of Minnesota
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.
Universita Degli Studi Di Firenze
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.
University of Trieste
Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy.
National Institute of Diabetes and Digestive and Kidney Diseases
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.
University of Ferrara
Exploring the 7-oxo-thiazolo[5,4-d]pyrimidine core for the design of new human adenosine A3 receptor antagonists. Synthesis, molecular modeling studies and pharmacological evaluation.
Universita' Di Firenze
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.
University of Ferrara
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
In vivo phenotypic screening for treating chronic neuropathic pain: modification of C2-arylethynyl group of conformationally constrained A3 adenosine receptor agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
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.
University of Florence
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.
University of Trieste
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
Synthesis and evaluation of N6-substituted apioadenosines as potential adenosine A3 receptor modulators.
Ghent University
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain.
University of Missouri
Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor.
Arena Pharmaceuticals
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.
University of Florence
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.
Universita Degli Studi Di Firenze
Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
The discovery of N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl)benzamide (SCH 900822): a potent and selective glucagon receptor antagonist.
Merck Research Laboratories
Flavonoid derivatives as adenosine receptor antagonists: a comparison of the hypothetical receptor binding site based on a comparative molecular field analysis model.
National Institute of Diabetes
Rational design of sulfonated A3 adenosine receptor-selective nucleosides as pharmacological tools to study chronic neuropathic pain.
National Institute of Diabetes and Digestive and Kidney Diseases
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
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.
University of Florence
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
Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions.
TBA
QSAR of adenosine receptor antagonists: Exploring physicochemical requirements for binding of pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives with human adenosine A(3) receptor subtype.
University Institute of Pharmaceutical Sciences and Ugc Center of Advanced Study In Pharmaceutical Sciences (Ugc-Cas)
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
Synthesis of novel 1-alkyl-8-substituted-3-(3-methoxypropyl) xanthines as putative A(2B) receptor antagonists.
Universidade De A Coru£A
Topological descriptors in modeling the agonistic activity of human A3 adenosine receptor ligands: the derivatives of 2-chloro-N(6)-substituted-4'-thioadenosine-5'-uronamide.
Sobhasaria Engineering College
Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor.
University of Bari Aldo Moro
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.
Universite£
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.
University of Trieste
Medicinal chemistry of A3 adenosine receptor modulators: pharmacological activities and therapeutic implications.
University of Ferrara
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
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
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.
University of Ferrara
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
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
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.
University of Pisa
Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.
TBA
Discovery of New Human A(2A) Adenosine Receptor Agonists: Design, Synthesis, and Binding Mode of Truncated 2-Hexynyl-4'-thioadenosine.
Ewha Womans University
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 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.
University of Pisa
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
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
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 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives.
Vernalis (R&D)
Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases.
Cv Therapeutics
1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A(2B) adenosine receptor antagonists.
University of Ferrara
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.
University of Bari Aldo Moro
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.
University of Camerino
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.
University of Pisa
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.
University of Ferrara
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.
University of Camerino
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.
University of Ferrara
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
Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.
National Institute of Diabetes and Digestive and Kidney Diseases
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.
University of Trieste
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.
University of Naples Federico II
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.
University of Urbino
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor.
Leiden/Amsterdam Center For Drug Research
Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists.
University of Camerino
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists.
University of Ferrara
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)
BCUT descriptors to predicting affinity toward A3 adenosine receptors.
Experimental Sugar Cane Station&Quot;Villa Clara-Cienfuegos&Quot
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
Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique adenosine derivative.
University of Bonn
Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists.
University of Ferrara
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.
Universita Degli Studi Di Firenze
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.
University of Ferrara
N6-substituted D-4'-thioadenosine-5'-methyluronamides: potent and selective agonists at the human A3 adenosine receptor.
Ewha Womans University
Ribose-modified nucleosides as ligands for adenosine receptors: synthesis, conformational analysis, and biological evaluation of 1'-C-methyl adenosine analogues.
University of Camerino
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary.
National Institute of Diabetes and Digestive and Kidney Diseases
2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor.
Leiden/Amsterdam Center For Drug Research
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A(2A)- and A(3)-adenosine receptor antagonists.
University of Bonn
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.
University of Camerino
Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists.
Vrije Universiteit
3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.
University of Pisa
Neoceptor concept based on molecular complementarity in GPCRs: a mutant adenosine A(3) receptor with selectively enhanced affinity for amine-modified nucleosides.
National Institute of Diabetes and Digestive and Kidney Diseases
Nucleosides and nucleotides. 200. Reinvestigation of 5'-N-ethylcarboxamidoadenosine derivatives: structure-activity relationships for P(3) purinoceptor-like proteins.
Hokkaido University
5'-O-alkyl ethers of N,2-substituted adenosine derivatives: partial agonists for the adenosine A1 and A3 receptors.
Leiden/Amsterdam Center For Drug Research
A novel class of highly potent and selective A1 adenosine antagonists: structure-affinity profile of a series of 1,8-naphthyridine derivatives.
University of Pisa
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.
National Institute of Diabetes
N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor.
Leiden/Amsterdam Center For Drug Research
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors.
Leiden University
Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
National Institute of Diabetes
Synthesis and biological activity of a new series of N6-arylcarbamoyl, 2-(Ar)alkynyl-N6-arylcarbamoyl, and N6-carboxamido derivatives of adenosine-5'-N-ethyluronamide as A1 and A3 adenosine receptor agonists.
University of Ferrara
Nucleosides and nucleotides. 177. 9-(6,7-dideoxy-beta-D-allo-hept-5- ynofuranosyl)adenine: a selective and potent ligand for P3 purinoceptor-like protein.
Hokkaido University
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies.
University of Camerino
Novel N6-(substituted-phenylcarbamoyl)adenosine-5'-uronamides as potent agonists for A3 adenosine receptors.
University of Ferrara
6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists.
National Institute of Diabetes
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors.
National Institute of Diabetes
Search for new purine- and ribose-modified adenosine analogues as selective agonists and antagonists at adenosine receptors.
National Institute of Diabetes
Structure-activity relationships of 9-alkyladenine and ribose-modified adenosine derivatives at rat A3 adenosine receptors.
National Institute of Diabetes
Structure-activity relationships of N6-benzyladenosine-5'-uronamides as A3-selective adenosine agonists.
National Institute of Diabetes
Selective ligands for rat A3 adenosine receptors: structure-activity relationships of 1,3-dialkylxanthine 7-riboside derivatives.
National Institute of Diabetes
2-Substitution of N6-benzyladenosine-5'-uronamides enhances selectivity for A3 adenosine receptors.
National Institute of Diabetes
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents.
Virginia Commonwealth University
Design, synthesis and binding affinity of 3'-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligands.
Seoul National University
7-Nitrobenzofurazan (NBD) derivatives of 5'-N-ethylcarboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors.
University of Pisa
Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor.
University of Camerino
Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications.
Niddk
2-Nitro analogues of adenosine and 1-deazaadenosine: synthesis and binding studies at the adenosine A1, A2A and A3 receptor subtypes.
University of Amsterdam
Fluorescent probes for adenosine receptors: synthesis and biology of N6-dansylaminoalkyl-substituted NECA derivatives.
Glaxowellcome Medicines Research Center
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.
University of Ferrara
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
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.
University of Ferrara
Synthesis, structure-affinity relationships, and molecular modeling studies of novel pyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.
Universita' Di Firenze
Pharmacophore elucidation for a new series of 2-aryl-pyrazolo-triazolo-pyrimidines as potent human A3 adenosine receptor antagonists.
National University of Singapore
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
The identification of the 2-phenylphthalazin-1(2H)-one scaffold as a new decorable core skeleton for the design of potent and selective human A3 adenosine receptor antagonists.
Universita` Degli Studi Di Firenze
Discovery of benzothiazole-based adenosine A2B receptor antagonists with improved A2A selectivity.
Roche Research Center
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
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
Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists.
Niddk
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
Spiroindolones, a potent compound class for the treatment of malaria.
Swiss Tropical and Public Health Institute
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
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
Synthesis and pharmacological characterization of a new series of 5,7-disubstituted-[1,2,4]triazolo[1,5-a][1,3,5]triazine derivatives as adenosine receptor antagonists: A preliminary inspection of ligand-receptor recognition process.
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
2-Dialkynyl derivatives of (N)-methanocarba nucleosides: 'Clickable' A(3) adenosine receptor-selective agonists.
Niddk
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
Nucleoside-5'-monophosphates as prodrugs of adenosine A2A receptor agonists activated by ecto-5'-nucleotidase.
University of Bonn
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.
University of Florence
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
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.
University of Padova
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)
A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor.
Leiden University
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
Novel 2- and 4-substituted 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric modulators of the A3 adenosine receptor.
National Institute of Diabetes and Digestive and Kidney Diseases
Synthesis, biological assays and QSAR studies of N-(9-benzyl-2-phenyl-8-azapurin-6-yl)-amides as ligands for A1 adenosine receptors.
Università
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
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
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists.
Ewha Womans University
Structure-activity relationships of 1,4-dihydropyridines that act as enhancers of the vanilloid receptor 1 (TRPV1).
National Institute of Diabetes and Digestive and Kidney Diseases
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
Ribose-modified purine nucleosides as ribonucleotide reductase inhibitors. Synthesis, antitumor activity, and molecular modeling of N6-substituted 3'-C-methyladenosine derivatives.
Università
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
N6-1,3-diphenylurea derivatives of 2-phenyl-9-benzyladenines and 8-azaadenines: synthesis and biological evaluation as allosteric modulators of A2A adenosine receptors.
Università
A small-molecule therapeutic lead for Huntington's disease: preclinical pharmacology and efficacy of C2-8 in the R6/2 transgenic mouse.
Harvard Medical School
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
Scouting human A3 adenosine receptor antagonist binding mode using a molecular simplification approach: from triazoloquinoxaline to a pyrimidine skeleton as a key study.
Università
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
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
Structure-Activity Relationship of Truncated 2,8-Disubstituted-Adenosine Derivatives as Dual A
Seoul National 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
Exploring the Effect of Halogenation in a Series of Potent and Selective A
University of Santiago de Compostela
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
Expanding the repertoire of methanocarba nucleosides from purinergic signaling to diverse targets.
National Institute of Diabetes & Digestive & Kidney Diseases
Optimization of a Screening Hit toward M2912, an Oral Tankyrase Inhibitor with Antitumor Activity in Colorectal Cancer Models.
Merck
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
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist.
Pfizer
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor.
Leiden University
Discovery of a Novel Class of d-Amino Acid Oxidase Inhibitors Using the Schrödinger Computational Platform.
Schr£Dinger
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
The synthesis of highly potent, selective, and water-soluble agonists at the human adenosine A3 receptor.
Pfizer
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
Synthesis and in vivo validation of [O-methyl-11C]2-{4-[4-(7-methoxynaphthalen-1-yl)piperazin- 1-yl]butyl}-4-methyl-2H-[1,2,4]triazine-3,5-dione: a novel 5-HT1A receptor agonist positron emission tomography ligand.
Columbia University College of Physicians and Surgeons
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
A topological function based on spectral moments for predicting affinity toward A3 adenosine receptors.
Vigo University
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
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
Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists.
Cv Therapeutics
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
Adenosine receptor antagonists: Recent advances and therapeutic perspective.
Isf College of Pharmacy
Discovery of Novel Allosteric EGFR L858R Inhibitors for the Treatment of Non-Small-Cell Lung Cancer as a Single Agent or in Combination with Osimertinib.
F. Hoffmann-La Roche
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
Structure-Activity Studies of 1
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
Combined target-based and ligand-based drug design approach as a tool to define a novel 3D-pharmacophore model of human A3 adenosine receptor antagonists: pyrazolo[4,3-e]1,2,4-triazolo[1,5-c]pyrimidine derivatives as a key study.
Università
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
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
Facile synthesis of fused 1,2,4-triazolo[1,5-c]pyrimidine derivatives as human adenosine A3 receptor ligands.
Otsuka Pharmaceutical Factory
2-(N-acyl) and 2-N-acyl-N(6)-substituted analogues of adenosine and their affinity at the human adenosine receptors.
Inotek Pharmaceuticals
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability.
University of Bonn
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
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
Design, synthesis and biological evaluation of novel N-alkyl- and N-acyl-(7-substituted-2-phenylimidazo[1,2-a][1,3,5]triazin-4-yl)amines (ITAs) as novel A(1) adenosine receptor antagonists.
Università
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)
Discovery and Structure-Activity Relationships of Novel Template, Truncated 1'-Homologated Adenosine Derivatives as Pure Dual PPARγ/δ Modulators.
Seoul National University
2-Aminothiazoles: a new class of agonist allosteric enhancers of A(1) adenosine receptors.
University of Virginia
Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions.
National Institute of Diabetes & Digestive & Kidney Diseases
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
Synthesis and purine receptor affinity of 6-oxopurine nucleosides and nucleotides containing (N)-methanocarba-pseudoribose rings.
Niddk
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
Universita Degli Studi Di Firenze
Structural investigation on thiazolo[5,4-d]pyrimidines to obtain dual-acting blockers of CD73 and adenosine A
Universita Degli Studi Di Firenze
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
Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor.
Leiden/Amsterdam Center For Drug Research
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
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
7-Deazaadenines bearing polar substituents: structure-activity relationships of new A(1) and A(3) adenosine receptor antagonists.
University of Leipzig
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
Synthesis and structure-activity relationships of a new set of 2-arylpyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists.
Universita' Di Firenze
8-Substituted 1,3-dimethyltetrahydropyrazino[2,1-f]purinediones: Water-soluble adenosine receptor antagonists and monoamine oxidase B inhibitors.
University of Bonn
Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor.
Vrije Universiteit
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors.
National Institute of Diabetes
1,2,4-Triazolo[4,3-a]quinoxalin-1-one: a versatile tool for the synthesis of potent and selective adenosine receptor antagonists.
Universita' Di Firenze
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
The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family.
Chembridge
Modifications on the Amino-3,5-dicyanopyridine Core To Obtain Multifaceted Adenosine Receptor Ligands with Antineuropathic Activity.
Universita Degli Studi Di Firenze
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 A(3) adenosine receptor antagonists: water-soluble 3, 5-diacyl-1,2,4-trialkylpyridinium salts and their oxidative generation from dihydropyridine precursors.
National Institute of Diabetes
Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.
National Institute of Diabetes
Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A
Leiden University
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs.
Universit£T Bonn
Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists.
National Institute of Diabetes
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Shanghaitech University
The synthesis of new adenosine A3 selective ligands containing bioisosteric isoxazoles.
Novo Nordisk
A novel class of adenosine A3 receptor ligands. 2. Structure affinity profile of a series of isoquinoline and quinazoline compounds.
Vrije Universiteit
A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives.
Vrije Universiteit
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes.
National Institute of Diabetes
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.
Universita Degli Studi Di Firenze
Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists.
National Institute of Diabetes
Structural Characterization of Agonist Binding to an A
National and Kapodistrian University of Athens
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.
National Institute of Diabetes
Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists.
National Institute of Diabetes
Structure-Based Design, Synthesis by Click Chemistry and
National Institute of Diabetes and Digestive and Kidney Diseases
Interactions of flavonoids and other phytochemicals with adenosine receptors.
National Institute of Diabetes
Tetrahydrobenzothiophenone derivatives as a novel class of adenosine receptor antagonists.
National Institute of Diabetes
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example.
Janssen Pharmaceutica
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 N²-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 A₂A adenosine receptor ligands.
University of Camerino
Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives.
University of Pisa
Structure-activity relationships of 1,3-dialkylxanthine derivatives at rat A3 adenosine receptors.
National Institute of Diabetes
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
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
QSAR of adenosine A3 receptor antagonist 1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives using chemometric tools.
Jadavpur University
[1,2,4]Triazolo[1,5-c]pyrimidines as adenosine receptor antagonists: Modifications at the 8 position to reach selectivity towards A
University of Trieste
Emerging Approaches for the Identification of Protein Targets of Small Molecules - A Practitioners' Perspective.
Abbvie
The aminopyridine-3,5-dicarbonitrile core for the design of new non-nucleoside-like agonists of the human adenosine A
Universita Degli Studi Di Firenze
Structure-activity relationship studies and pharmacological characterization of N
Universita Degli Studi Di Firenze
Identification of novel thiazolo[5,4-d]pyrimidine derivatives as human A
Universita Degli Studi Di Firenze
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 RORγt.
Phenex Pharmaceuticals
Development of novel pyridazinone-based adenosine receptor ligands.
Universita Degli Studi Di Firenze
Structure-Based Design, Synthesis, and In Vivo Antinociceptive Effects of Selective A
University of Camerino
Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A
Leiden University
SALT FORM AND CRYSTAL FORM OF PYRAZOLE SUBSTITUTED IMIDAZO[1,2- A]QUINOXALINE DERIVATIVE
Ocumension Therapeutics (Suzhou) Co.
Oral compositions of MK2 pathway inhibitor for treatment of immune conditions
Aclaris Therapeutics
Substituted N-pyrimidin-4-yl-3-aminopyrrolo[3,4-C]pyrazoles as protein kinase C inhibitors
Pfizer
Tosylacetate based compounds and derivatives thereof as PHGDH inhibitors
Boehringer Ingelheim International
1,2-dithiolane compounds useful in neuroprotection, autoimmune and cancer diseases and conditions
Sabila Biosciences
Inhibitors of ADAMTS4 or ADAMTS5 for use in preventing or treating cardiac remodeling and chronic heart failure
Universitetet I Oslo
Transformation of the Non-Selective Aminocyclohexanol-Based Hsp90 Inhibitor into a Grp94-Seletive Scaffold.
The University of Kansas
Rationally designed sulfamides as glutamate carboxypeptidase II inhibitors.
Washington State University At Pullman
Aryl- and heteroarylcarbonyl derivatives of hexahydroindenopyridine and octahydrobenzoquinoline
Vitae Pharmaceuticals
Altered enthalpy-entropy compensation in picomolar transition state analogues of human purine nucleoside phosphorylase.
Albert Einstein College of Medicine
Neoflavonoids and Tetrahydroquinolones as Possible Cancer Chemopreventive Agents.
Central Institute of Medicinal and Aromatic Plants
Intersubunit bridge formation governs agonist efficacy at nicotinic acetylcholine α4β2 receptors: unique role of halogen bonding revealed.
University of Copenhagen
Molecular cloning and characterization of the human A3 adenosine receptor.
Merck Research Laboratories
Glycogen phosphorylase inhibitory effects of 2-oxo-1,2-dihydropyridin-3-yl amide derivatives.
Griffith University
Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase.
Northern Kentucky University
Discovery of antibacterial biotin carboxylase inhibitors by virtual screening and fragment-based approaches.
Pfizer
Design, synthesis and structure-activity relationships of 1,3,4-oxadiazole derivatives as novel inhibitors of glycogen synthase kinase-3beta.
Takeda Pharmaceutical
Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064.
Gsk
Tacripyrines, the first tacrine-dihydropyridine hybrids, as multitarget-directed ligands for the treatment of Alzheimer's disease.
Csic
Interaction of papain-like cysteine proteases with dipeptide-derived nitriles.
Rheinische Friedrich-Wilhelms-Universitat Bonn
Discovery of CGS 27023A, a non-peptidic, potent, and orally active stromelysin inhibitor that blocks cartilage degradation in rabbits.
Novartis Pharmaceuticals