The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 28590753 |
162 |
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£ |
| 28380296 |
64 |
N |
Seoul National University |
| 28055204 |
74 |
Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine A |
Advinus Therapeutics |
| 27842891 |
75 |
A |
Advinus Therapeutics |
| 28238512 |
54 |
Design and synthesis of novel, potent and selective hypoxanthine analogs as adenosine A |
Advinus Therapeutics |
| 27933962 |
89 |
Design, Synthesis, and Pharmacological Characterization of 2-(2-Furanyl)thiazolo[5,4-d]pyrimidine-5,7-diamine Derivatives: New Highly Potent A |
Universit£ |
| 27718474 |
40 |
Synthesis and evaluation of N-substituted 2-amino-4,5-diarylpyrimidines as selective adenosine A |
Leiden University |
| 27876250 |
60 |
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 |
| 27994726 |
19 |
Quinazoline Carboxamides as Selective Antagonists of Adenosine 2A Receptor. |
Dart Neuroscience |
| 27933955 |
123 |
Biphenyl Pyridazinone Derivatives as Inhaled PDE4 Inhibitors: Structural Biology and Structure-Activity Relationships. |
RhôNe-Poulenc Rorer |
| 27933810 |
166 |
Structure-Based Scaffold Repurposing for G Protein-Coupled Receptors: Transformation of Adenosine Derivatives into 5HT |
National Institute of Diabetes and Digestive and Kidney Diseases |
| 27227326 |
156 |
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 |
| 27485602 |
183 |
Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine receptors. |
Jagiellonian University Medical College |
| 27124340 |
10 |
5'-Substituted Amiloride Derivatives as Allosteric Modulators Binding in the Sodium Ion Pocket of the Adenosine A2A Receptor. |
Leiden University |
| 27161878 |
83 |
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£ |
| 26824742 |
43 |
Discovery of Potent and Highly Selective A2B Adenosine Receptor Antagonist Chemotypes. |
Uppsala University |
| 26988801 |
55 |
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 |
| 26756468 |
44 |
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity. |
University of Warwick |
| 26356532 |
39 |
Discovery of Molecular Therapeutics for Glaucoma: Challenges, Successes, and Promising Directions. |
Georgia Institute of Technology |
| 26781932 |
109 |
Discovery of aminoquinazoline derivatives as human A(2A) adenosine receptor antagonists. |
Merck Research Laboratories |
| 26638043 |
66 |
Structural refinement of pyrazolo[4,3-d]pyrimidine derivatives to obtain highly potent and selective antagonists for the human A3 adenosine receptor. |
Universit£ |
| 26717203 |
129 |
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£ |
| 26048804 |
57 |
Use of molecular modeling aided design to dial out hERG liability in adenosine A(2A) receptor antagonists. |
Merck Research Laboratories |
| 26046697 |
46 |
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£ |
| 25969169 |
54 |
A solid-phase combinatorial approach for indoloquinolizidine-peptides with high affinity at D(1) and D(2) dopamine receptors. |
University of Barcelona |
| 25780876 |
205 |
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£ |
| 25699637 |
91 |
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 |
| 25633494 |
128 |
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 |
| 25701253 |
23 |
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 |
| 25686851 |
54 |
Novel thiazole-thiophene conjugates as adenosine receptor antagonists: synthesis, biological evaluation and docking studies. |
B. V. Patel Pharmaceutical Education and Research Development (Perd) Centre |
| 25490054 |
92 |
Synthesis and pharmacological evaluation of dual acting ligands targeting the adenosine A2A and dopamine D2 receptors for the potential treatment of Parkinson's disease. |
Monash University (Parkville Campus) |
| 25063944 |
56 |
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£ |
| 24972108 |
256 |
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£ |
| 24969016 |
16 |
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 |
| 24881566 |
140 |
Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). |
Glaxosmithkline |
| 24863744 |
15 |
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
University of Missouri |
| 25497490 |
30 |
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£ |
| 25462223 |
27 |
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£ |
| 25349648 |
29 |
Discovery of a Potent and Selective DGAT1 Inhibitor with a Piperidinyl-oxy-cyclohexanecarboxylic Acid Moiety. |
Merck Research Laboratories |
| 25221664 |
21 |
Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor. |
National Institute of Diabetes and Digestive and Kidney Diseases |
| 24815000 |
21 |
8-Substituted 2-alkynyl-N(9)-propargyladenines as A2A adenosine receptor antagonists. |
Yamasa |
| 24164628 |
186 |
Adenosine A2A receptor as a drug discovery target. |
Merck Research Laboratories |
| 24669958 |
39 |
Agonists for the adenosine A1 receptor with tunable residence time. A Case for nonribose 4-amino-6-aryl-5-cyano-2-thiopyrimidines. |
Leiden University |
| 23597047 |
5 |
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 |
| 23427825 |
45 |
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£ |
| 23245803 |
87 |
Synthesis and structure-activity relationships of 2-hydrazinyladenosine derivatives as A(2A) adenosine receptor ligands. |
University of Bonn |
| 24900549 |
6 |
Metabolites of the pyrimidine amine preladenant as adenosine a2a receptor antagonists. |
Dart Neuroscience |
| 23281824 |
118 |
Synthesis of (E)-8-(3-chlorostyryl)caffeine analogues leading to 9-deazaxanthine derivatives as dual A(2A) antagonists/MAO-B inhibitors. |
Universit£ |
| 23231967 |
23 |
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 |
| 23171656 |
23 |
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 |
| 23145215 |
23 |
Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions. |
TBA |
| 21661720 |
8 |
Biophysical mapping of the adenosine A2A receptor. |
Heptares Therapeutics |
| 20371139 |
16 |
Synthesis and pharmacological evaluation of novel substituted 9-deazaxanthines as A2B receptor antagonists. |
Universidade De A Coru£A |
| 20382540 |
9 |
In silico directed chemical probing of the adenosine receptor family. |
Universidade Do Minho |
| 20137957 |
35 |
Synthesis and pharmacological evaluation of novel 1,3,8- and 1,3,7,8-substituted xanthines as adenosine receptor antagonists. |
Universidade De Porto |
| 19682912 |
80 |
Synthesis and pharmacological evaluation of novel 1- and 8-substituted-3-furfuryl xanthines as adenosine receptor antagonists. |
Universidade De Santiago De Compostela |
| 19346133 |
58 |
Synthesis of novel 1-alkyl-8-substituted-3-(3-methoxypropyl) xanthines as putative A(2B) receptor antagonists. |
Universidade De A Coru£A |
| 16392813 |
329 |
Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor. |
Universit£ |
| 23098605 |
248 |
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£ |
| 22468757 |
171 |
Medicinal chemistry of A3 adenosine receptor modulators: pharmacological activities and therapeutic implications. |
Universit£ |
| 22921089 |
62 |
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 |
| 22827545 |
11 |
Identifying novel adenosine receptor ligands by simultaneous proteochemometric modeling of rat and human bioactivity data. |
Leiden/Amsterdam Center For Drug Research |
| 22738238 |
29 |
Orally active adenosine A(1) receptor agonists with antinociceptive effects in mice. |
University of North Carolina At Chapel Hill |
| 22239465 |
26 |
Design and characterization of optimized adenosine A2A/A1 receptor antagonists for the treatment of Parkinson's disease. |
Janssen Research and Development |
| 21664729 |
142 |
Synthesis and biological activity of tricyclic cycloalkylimidazo-, pyrimido- and diazepinopurinediones. |
Jagiellonian University Medical College |
| 23342198 |
77 |
Structure-activity relationships and molecular modeling of 1,2,4-triazoles as adenosine receptor antagonists. |
TBA |
| 22568637 |
158 |
Water-soluble pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidines as human A3 adenosine receptor antagonists. |
Universit£ |
| 22563707 |
27 |
A prospective cross-screening study on G-protein-coupled receptors: lessons learned in virtual compound library design. |
Radboud University Nijmegen Medical Centre |
| 22486652 |
44 |
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 |
| 22559880 |
52 |
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 |
| 22677030 |
29 |
New chromene scaffolds for adenosine A(2A) receptors: synthesis, pharmacology and structure-activity relationships. |
Universidade Do Minho |
| 22432713 |
64 |
Synthesis and pharmacological evaluation of dual acting antioxidant A(2A) adenosine receptor agonists. |
Monash University |
| 24900277 |
36 |
Development of Polar Adenosine A2A Receptor Agonists for Inflammatory Bowel Disease: Synergism with A2B Antagonists. |
TBA |
| 22257095 |
65 |
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£ |
| 22250781 |
16 |
Identification of novel adenosine A(2A) receptor antagonists by virtual screening. |
Heptares Therapeutics |
| 22220592 |
27 |
Discovery of 1,2,4-triazine derivatives as adenosine A(2A) antagonists using structure based drug design. |
Heptares Therapeutics |
| 22148921 |
48 |
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c |
Cephalon |
| 21858244 |
62 |
Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element. |
TBA |
| 21286238 |
9 |
Discovery of New Human A(2A) Adenosine Receptor Agonists: Design, Synthesis, and Binding Mode of Truncated 2-Hexynyl-4'-thioadenosine. |
Ewha Womans University |
| 21210664 |
74 |
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 |
| 20875743 |
90 |
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 |
| 20931963 |
112 |
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 |
| 20684563 |
176 |
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 |
| 20541935 |
131 |
4-Substituted-7-N-alkyl-N-acetyl 2-aminobenzothiazole amides: drug-like and non-xanthine based A2B adenosine receptor antagonists. |
Roche Research Center |
| 20408530 |
98 |
Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation. |
Universit£ |
| 20303771 |
24 |
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 |
| 20188574 |
141 |
2-Amino-5-benzoyl-4-phenylthiazoles: Development of potent and selective adenosine A1 receptor antagonists. |
University of Bonn |
| 19569717 |
251 |
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 |
| 19282184 |
195 |
8-Bromo-9-alkyl adenine derivatives as tools for developing new adenosine A2A and A2B receptors ligands. |
University of Camerino |
| 18637670 |
80 |
2-Amino-6-furan-2-yl-4-substituted nicotinonitriles as A2A adenosine receptor antagonists. |
Leiden/Amsterdam Center For Drug Research |
| 18262425 |
27 |
Synthesis of eudistomin D analogues and its effects on adenosine receptors. |
Hokkaido University |
| 18424135 |
131 |
Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists. |
National Institute of Diabetes and Digestive and Kidney Diseases |
| 18411049 |
134 |
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) |
| 18407496 |
127 |
Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives. |
Vernalis (R&D) |
| 18406614 |
56 |
Antagonists of the human adenosine A2A receptor. Part 1: Discovery and synthesis of thieno[3,2-d]pyrimidine-4-methanone derivatives. |
Vernalis (R&D) |
| 18321039 |
144 |
Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases. |
Cv Therapeutics |
| 18321038 |
85 |
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 |
| 18077171 |
108 |
1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A(2B) adenosine receptor antagonists. |
Universit£ |
| 18258439 |
69 |
A new generation of adenosine receptor antagonists: from di- to trisubstituted aminopyrimidines. |
Leiden/Amsterdam Center For Drug Research |
| 18226909 |
162 |
1-, 3- and 8-substituted-9-deazaxanthines as potent and selective antagonists at the human A2B adenosine receptor. |
Universit£ |
| 17483457 |
58 |
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat. |
Abbott Laboratories |
| 18255292 |
35 |
Structure-activity relationships of 2-chloro-N6-substituted-4'-thioadenosine-5'-N,N-dialkyluronamides as human A3 adenosine receptor antagonists. |
Ewha Womans University |
| 18249540 |
28 |
2,6-Diaryl-4-phenacylaminopyrimidines as potent and selective adenosine A(2A) antagonists with reduced hERG liability. |
Neurocrine Biosciences |
| 18243699 |
11 |
Inhaled adenosine A(2A) receptor agonists for the treatment of chronic obstructive pulmonary disease. |
Pfizer |
| 18181565 |
71 |
Multi-target-directed ligands to combat neurodegenerative diseases. |
University of Bologna |
| 17933541 |
145 |
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£ |
| 17967536 |
34 |
Structure-activity relationships of adenosines with heterocyclic N6-substituents. |
Monash University (Parkville Campus) |
| 17927167 |
107 |
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£ |
| 17306548 |
84 |
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£ |
| 17378544 |
121 |
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 |
| 17309246 |
108 |
N6-methoxy-2-alkynyladenosine derivatives as highly potent and selective ligands at the human A3 adenosine receptor. |
Universit£ |
| 17228880 |
76 |
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£ |
| 17228876 |
36 |
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 |
| 17201410 |
4 |
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 |
| 16487705 |
107 |
N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists. |
University of Virginia |
| 16509587 |
72 |
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£ |
| 16366607 |
81 |
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£ |
| 16250647 |
71 |
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£ |
| 15771447 |
24 |
A series of ligands displaying a remarkable agonistic-antagonistic profile at the adenosine A1 receptor. |
Leiden/Amsterdam Center For Drug Research |
| 15743197 |
37 |
Synthesis, biological evaluation, and molecular modeling of ribose-modified adenosine analogues as adenosine receptor agonists. |
Universit£ |
| 15481989 |
70 |
Synthesis and biological evaluation of novel N6-[4-(substituted)sulfonamidophenylcarbamoyl]adenosine-5'-uronamides as A3 adenosine receptor agonists. |
Universit£ |
| 15341491 |
62 |
2-Pyrazolyl-N(6)-substituted adenosine derivatives as high affinity and selective adenosine A(3) receptor agonists. |
Cv Therapeutics |
| 15267242 |
54 |
Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor. |
Iiqab (Csic) |
| 15876531 |
28 |
A new orally bioavailable dual adenosine A2B/A3 receptor antagonist with therapeutic potential. |
Novartis Institutes For Biomedical Research |
| 15341938 |
6 |
Design and synthesis of 3'-ureidoadenosine-5'-uronamides: effects of the 3'-ureido group on binding to the A3 adenosine receptor. |
Ewha Womans University |
| 14998332 |
328 |
Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists. |
Universit£ |
| 15239649 |
24 |
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 |
| 15214785 |
58 |
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£ |
| 12672250 |
10 |
N6-cyclopentyl-2-(3-phenylaminocarbonyltriazene-1-yl)adenosine (TCPA), a very selective agonist with high affinity for the human adenosine A1 receptor. |
Leiden University |
| 12646033 |
124 |
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£ |
| 14584936 |
39 |
Modeling the adenosine receptors: comparison of the binding domains of A2A agonists and antagonists. |
Niddk |
| 12383013 |
44 |
Synthesis, molecular modeling studies, and pharmacological activity of selective A(1) receptor antagonists. |
Universit£ |
| 11784146 |
9 |
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 |
| 12109910 |
8 |
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£ |
| 11462973 |
47 |
3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists. |
Universit£ |
| 10956189 |
98 |
A novel class of highly potent and selective A1 adenosine antagonists: structure-affinity profile of a series of 1,8-naphthyridine derivatives. |
Universit£ |
| 10841798 |
64 |
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists. |
National Institute of Diabetes |
| 10212124 |
26 |
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors. |
Leiden University |
| 9572897 |
49 |
2'-C-Methyl analogues of selective adenosine receptor agonists: synthesis and binding studies. |
Universit£ |
| 9258366 |
41 |
Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors. |
Niddk |
| 8258836 |
3 |
Synthesis and biological evaluation of N4-substituted imidazo- and v-triazolo[4,5-d]pyridazine nucleosides. |
University of Rhode Island |
| 11714602 |
18 |
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Ewha Womans University |
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Aix-Marseille Universit£ |
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Ewha Womans University |
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Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists. |
Ewha Womans University |
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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 |
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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 |
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Dual acting antioxidant A1 adenosine receptor agonists. |
Monash University (Parkville Campus) |
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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 |
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Novel ergopeptides as dual ligands for adenosine and dopamine receptors. |
Institut D'Investigacions BiomèDiques August Pi I |
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Jagiellonian University |
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Biogen Idec |
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Leiden University |
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2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. |
Leiden/Amsterdam Center For Drug Research |
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Ewha Womans University |
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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 |
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National Institute of Diabetes and Digestive and Kidney Diseases |
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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 |
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National Institute of Diabetes and Digestive and Kidney Diseases |
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6-(2-Furanyl)-9H-purin-2-amine derivatives as A2A adenosine antagonists. |
Schering-Plough Research Institute |
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Leiden/Amsterdam Center For Drug Research |
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TBA |
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Instituto De QuíMica MéDica (Csic) |
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University of Virginia |
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University of Bonn |
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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 |
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Synthesis and biological data of 4-amino-1-(2-chloro-2-phenylethyl)-1H-pyrazolo[3,4-b]pyridine-5-carboxylic acid ethyl esters, a new series of A1-adenosine receptor (A1AR) ligands. |
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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 |
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Structural investigation on thiazolo[5,4-d]pyrimidines to obtain dual-acting blockers of CD73 and adenosine A |
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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. |
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Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent A |
Uppsala University |
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Eisai |
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Università |
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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 |
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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 |
| 10956220 |
93 |
Synthesis and structure-activity relationships of a new set of 2-arylpyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists. |
Universita' Di Firenze |
| 27658798 |
376 |
8-Substituted 1,3-dimethyltetrahydropyrazino[2,1-f]purinediones: Water-soluble adenosine receptor antagonists and monoamine oxidase B inhibitors. |
University of Bonn |
| 27312113 |
10 |
Controlling the Dissociation of Ligands from the Adenosine A2A Receptor through Modulation of Salt Bridge Strength. |
Heptares Therapeutics |
| 30576906 |
92 |
Novel non-xanthine antagonist of the A |
Bayer Pharmaceuticals |
| 31855793 |
72 |
Identification of new potent A |
Nankai University |
| 10737749 |
182 |
Anilide derivatives of an 8-phenylxanthine carboxylic congener are highly potent and selective antagonists at human A(2B) adenosine receptors. |
National Institute of Diabetes |
| 10737748 |
81 |
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 |
| 31557025 |
100 |
Trifluorinated Pyrimidine-Based A |
Uppsala University |
| 31404862 |
138 |
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases. |
Palack£ |
| 10698437 |
7 |
Synthesis and preliminary biological evaluation of [3H]-MRE 3008-F20: the first high affinity radioligand antagonist for the human A3 adenosine receptors. |
Università |
| 10669571 |
24 |
Water-soluble phosphate prodrugs of 1-propargyl-8-styrylxanthine derivatives, A(2A)-selective adenosine receptor antagonists. |
University of WüRzburg |
| 31306001 |
117 |
Modifications on the Amino-3,5-dicyanopyridine Core To Obtain Multifaceted Adenosine Receptor Ligands with Antineuropathic Activity. |
Universit£ |
| 31298539 |
18 |
Design, Synthesis, and Characterization of Ogerin-Based Positive Allosteric Modulators for G Protein-Coupled Receptor 68 (GPR68). |
Icahn School of Medicine At Mount Sinai |
| 32271569 |
76 |
Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A |
Medical College of Wisconsin |
| 10579811 |
70 |
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 |
| 10476879 |
52 |
Selective A1-adenosine receptor antagonists identified using yeast Saccharomyces cerevisiae functional assays. |
Cadus Pharmaceutical |
| 30952592 |
206 |
Accelerating the discovery of DGAT1 inhibitors through the application of parallel medicinal chemistry (PMC). |
Merck |
| 30869893 |
26 |
Development of Covalent Ligands for G Protein-Coupled Receptors: A Case for the Human Adenosine A |
Leiden University |
| 31280999 |
29 |
2-Aryladenine derivatives as a potent scaffold for A |
Universidade Do Minho |
| 31846328 |
8 |
Docking Finds GPCR Ligands in Dark Chemical Matter. |
Uppsala University |
| 31738058 |
154 |
Structure-Based Optimization of Coumarin hA |
University of Porto |
| 30605331 |
236 |
Design and in Vivo Characterization of A |
Medical College of Wisconsin |
| 31185168 |
144 |
Functionalized 6-(Piperidin-1-yl)-8,9-Diphenyl Purines as Peripherally Restricted Inverse Agonists of the CB1 Receptor. |
Rti International |
| 31255928 |
82 |
Design, synthesis and biological evaluation of 2-hydrazinyladenosine derivatives as A |
National Engineering Research Center For The Emergency Drug |
| 30835463 |
202 |
A |
Rheinische Friedrich-Wilhelms-Universitat Bonn |
| 30826188 |
25 |
Thieno[2,3-d]pyrimidine as a promising scaffold in medicinal chemistry: Recent advances. |
University of Science & Technology (Ust) |
| 9622554 |
59 |
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 |
| 30638876 |
108 |
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£ |
| 31453698 |
97 |
Antioxidant-Conjugated 1,2,4-Triazolo[4,3- |
Universit£ |
| 8863790 |
55 |
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype. |
National Institute of Diabetes |
| 26592528 |
37 |
Fragment-Based Discovery of Subtype-Selective Adenosine Receptor Ligands from Homology Models. |
Stockholm University |
| 26236460 |
36 |
Structure-Based Design, Synthesis by Click Chemistry and |
National Institute of Diabetes and Digestive and Kidney Diseases |
| 26513641 |
14 |
Design and synthesis of fused tetrahydroisoquinoline-iminoimidazolines. |
Universit£ |
| 26565745 |
165 |
Benzazaborinines as Novel Bioisosteric Replacements of Naphthalene: Propranolol as an Example. |
Janssen Pharmaceutica |
| 24456490 |
33 |
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 |
| 24556147 |
52 |
Novel 8-(p-substituted-phenyl/benzyl)xanthines with selectivity for the A2A adenosine receptor possess bronchospasmolytic activity. |
Panjab University |
| 24518296 |
119 |
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 |
| 24332624 |
12 |
Replacement of amide with bioisosteres led to a new series of potent adenosine A2A receptor antagonists. |
Soochow University |
| 24139167 |
419 |
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 |
| 24900602 |
32 |
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 |
| 24189496 |
67 |
8-(2-Furyl)adenine derivatives as A?A adenosine receptor ligands. |
University of Camerino |
| 8071944 |
37 |
8-Azaxanthine derivatives as antagonists of adenosine receptors. |
Università |
| 24077183 |
32 |
Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives. |
Universit£ |
| 23953686 |
28 |
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 |
| 23789814 |
22 |
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£ |
| 23685887 |
80 |
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 |
| 23631427 |
212 |
Dual targeting of adenosine A(2A) receptors and monoamine oxidase B by 4H-3,1-benzothiazin-4-ones. |
University of Bonn |
| 23602401 |
50 |
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) |
| 23522563 |
94 |
Substituted thieno[2,3-d]pyrimidines as adenosine A2A receptor antagonists. |
Janssen Research & Development |
| 18249548 |
62 |
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 |
| 30144700 |
176 |
[1,2,4]Triazolo[1,5-c]pyrimidines as adenosine receptor antagonists: Modifications at the 8 position to reach selectivity towards A |
Universit£ |
| 29268131 |
32 |
Antagonists of the adenosine A |
Umr-S1172 - Jparc - Centre De Recherche Jean-Pierre Aubert Neurosciences Et Cancer |
| 29525433 |
41 |
The aminopyridine-3,5-dicarbonitrile core for the design of new non-nucleoside-like agonists of the human adenosine A |
Universit£ |
| 28835798 |
68 |
Discovery of Potent and Selective A |
Advinus Therapeutics |
| 29681156 |
71 |
Fluorescent-Labeled Selective Adenosine A |
University of Bonn |
| 29909340 |
90 |
Structure-activity relationship studies and pharmacological characterization of N |
Universit£ |
| 29614417 |
110 |
New potent and selective A |
University of Camerino |
| 2724296 |
113 |
Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions. |
National Institutes of Health |
| 30080404 |
9 |
An Affinity-Based Probe for the Human Adenosine A |
Astrazeneca |
| 29880250 |
84 |
Identification of novel thiazolo[5,4-d]pyrimidine derivatives as human A |
Universit£ |
| 29792714 |
32 |
Docking Screens for Dual Inhibitors of Disparate Drug Targets for Parkinson's Disease. |
Uppsala University |
| 29753566 |
19 |
Design and synthesis of 2,6-disubstituted-8-amino imidazo[1,2a]pyridines, a promising privileged structure. |
Universities of Lille |
| 29631962 |
252 |
Identification and biological evaluation of thiazole-based inverse agonists of ROR?t. |
Phenex Pharmaceuticals |
| 29627261 |
15 |
Development of novel pyridazinone-based adenosine receptor ligands. |
Universit£ |
| 28447789 |
134 |
Exploring the Role of N |
University of Camerino |
| 28374589 |
73 |
Indazole-6-phenylcyclopropylcarboxylic Acids as Selective GPR120 Agonists with in Vivo Efficacy. |
Astrazeneca |
| 28368607 |
26 |
Enantiospecific Recognition at the A |
Uppsala University |
| 29446948 |
82 |
A Structure-Activity Relationship Study of Bitopic N |
Monash University |
| 28807572 |
74 |
Identification of highly selective and potent orexin receptor 1 antagonists derived from a dual orexin receptor 1/2 antagonist based on the structural framework of pyrazoylethylbenzamide. |
Taisho Pharmaceutical |
| 27721147 |
30 |
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 |
| 28792759 |
22 |
Effect of Nitrogen Atom Substitution in A |
Uppsala University |
| 28626529 |
12 |
Photoaffinity Labeling of the Human A |
Kissei Pharmaceutical |
| 29257884 |
75 |
Structure-Based Design, Synthesis, and In Vivo Antinociceptive Effects of Selective A |
University of Camerino |
| 28799755 |
51 |
Polypharmacology of N |
Sahmyook University |
| 1331453 |
106 |
Effects of alkyl substitutions of xanthine skeleton on bronchodilation. |
Hokuriku University |
| 28238723 |
39 |
Non-steroidal Anti-inflammatory Drugs Are Caspase Inhibitors. |
University of Colorado |
| 26833890 |
18 |
Synthesis, Biological Evaluation, and Molecular Docking of 8-imino-2-oxo-2H,8H-pyrano[2,3-f]chromene Analogs: New Dual AChE Inhibitors as Potential Drugs for the Treatment of Alzheimer's Disease. |
Yogi Vemana University |
| 26440714 |
28 |
Synthesis, cholinesterase inhibition and molecular modelling studies of coumarin linked thiourea derivatives. |
Quaid-I-Azam University |
| 26432614 |
18 |
Synthesis, in vitro evaluation and molecular docking studies of biscoumarin thiourea as a new inhibitor of a-glucosidases. |
Universiti Teknologi Mara |
| 26469307 |
7 |
Phosphorylation of Capsaicinoid Derivatives Provides Highly Potent and Selective Inhibitors of the Transcription Factor STAT5b. |
University of Leipzig |
| 12110997 |
380 |
In vitro receptor screening of pure constituents of St. John's wort reveals novel interactions with a number of GPCRs. |
WestfÄLische Wilhelms-UniversitÄ |
| 6087359 |
69 |
Psychotomimetic opiate receptors labeled and visualized with (+)-[3H]3-(3-hydroxyphenyl)-N-(1-propyl)piperidine. |
TBA |
| 19880322 |
56 |
N-acylpolyamine inhibitors of HDM2 and HDMX binding to p53. |
Nih |
| 18215016 |
6 |
Design, Synthesis, Evaluation, and Crystallographic-Based Structural Studies of HIV-1 Protease Inhibitors with Reduced Response to the V82A Mutation. |
Universidad De Santiago De Compostela |
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