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£ |
28621538 |
63 |
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo. |
Novartis Pharma |
28380296 |
64 |
N |
Seoul National University |
28055204 |
74 |
Design, Synthesis of Novel, Potent, Selective, Orally Bioavailable Adenosine 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£ |
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 |
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 |
27128178 |
9 |
1'-Homonucleosides and their structural analogues: A review. |
Medical University of Lodz |
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 |
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 |
26390077 |
42 |
Tactical Approaches to Interconverting GPCR Agonists and Antagonists. |
University of Minnesota |
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£ |
26191370 |
34 |
Rigidified A3 Adenosine Receptor Agonists: 1-Deazaadenine Modification Maintains High in Vivo Efficacy. |
National Institute of Diabetes and Digestive and Kidney Diseases |
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£ |
25874336 |
16 |
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 |
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 |
25422861 |
78 |
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 |
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 |
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£ |
25019478 |
13 |
Flavones: an important scaffold for medicinal chemistry. |
Punjabi University |
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 |
24931275 |
6 |
Synthesis and evaluation of N6-substituted apioadenosines as potential adenosine A3 receptor modulators. |
Ghent University |
24863744 |
15 |
DDD-028: a potent potential non-opioid, non-cannabinoid analgesic for neuropathic and inflammatory pain. |
University of Missouri |
25516790 |
37 |
Discovery of APD334: Design of a Clinical Stage Functional Antagonist of the Sphingosine-1-phosphate-1 Receptor. |
Arena Pharmaceuticals |
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£ |
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 |
24164628 |
186 |
Adenosine A2A receptor as a drug discovery target. |
Merck Research Laboratories |
24527772 |
262 |
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 |
9438021 |
97 |
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 |
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 |
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 |
22277057 |
11 |
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 |
23145215 |
23 |
Truncated Nucleosides as A(3) Adenosine Receptor Ligands: Combined 2-Arylethynyl and Bicyclohexane Substitutions. |
TBA |
21163647 |
121 |
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) |
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 |
19346133 |
58 |
Synthesis of novel 1-alkyl-8-substituted-3-(3-methoxypropyl) xanthines as putative A(2B) receptor antagonists. |
Universidade De A Coru£A |
18973967 |
39 |
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 |
16392813 |
329 |
Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor. |
Universit£ |
21381769 |
56 |
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery. |
Universite£ |
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 |
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£ |
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 |
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£ |
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 |
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£ |
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 |
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) |
18321039 |
144 |
Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases. |
Cv Therapeutics |
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 |
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£ |
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 |
16640329 |
50 |
Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists. |
National Institute of Diabetes and Digestive and Kidney Diseases |
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£ |
15771453 |
22 |
Development of spin-labeled probes for adenosine receptors. |
University of Bonn |
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 |
15084123 |
24 |
Novel amino acid derived natural products from the ascidian Atriolum robustum: identification and pharmacological characterization of a unique adenosine derivative. |
University of Bonn |
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£ |
12238926 |
99 |
Structural determinants of A(3) adenosine receptor activation: nucleoside ligands at the agonist/antagonist boundary. |
National Institute of Diabetes and Digestive and Kidney Diseases |
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 |
12139454 |
56 |
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 |
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£ |
11262085 |
92 |
Thiazole and thiadiazole analogues as a novel class of adenosine receptor antagonists. |
Vrije Universiteit |
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£ |
11708915 |
52 |
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 |
11585444 |
295 |
From hit to lead. Analyzing structure-profile relationships. |
Universities of Lille |
11520205 |
4 |
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 |
10841798 |
64 |
Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists. |
National Institute of Diabetes |
10212125 |
14 |
N6,5'-Disubstituted adenosine derivatives as partial agonists for the human adenosine A3 receptor. |
Leiden/Amsterdam Center For Drug Research |
10212124 |
26 |
5'-N-substituted carboxamidoadenosines as agonists for adenosine receptors. |
Leiden University |
9703464 |
40 |
Structure-activity relationships and molecular modeling of 3, 5-diacyl-2,4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists. |
National Institute of Diabetes |
8917655 |
72 |
6-phenyl-1,4-dihydropyridine derivatives as potent and selective A3 adenosine receptor antagonists. |
National Institute of Diabetes |
8709132 |
92 |
Interaction of 1,4-dihydropyridine and pyridine derivatives with adenosine receptors: selectivity for A3 receptors. |
National Institute of Diabetes |
15203136 |
39 |
(+/-)8-Amino-5,6,7,8-tetrahydroisoquinolines as novel antinociceptive agents. |
Virginia Commonwealth University |
12617898 |
13 |
Design, synthesis and binding affinity of 3'-fluoro analogues of Cl-IB-MECA as adenosine A3 receptor ligands. |
Seoul National University |
11714602 |
18 |
7-Nitrobenzofurazan (NBD) derivatives of 5'-N-ethylcarboxamidoadenosine (NECA) as new fluorescent probes for human A(3) adenosine receptors. |
Universit£ |
11459663 |
19 |
Introduction of alkynyl chains on C-8 of adenosine led to very selective antagonists of the A(3) adenosine receptor. |
Universit£ |
11392549 |
45 |
Ring-Constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5'-uronamide and 2'-deoxy modifications. |
Niddk |
10999489 |
29 |
2-Nitro analogues of adenosine and 1-deazaadenosine: synthesis and binding studies at the adenosine A1, A2A and A3 receptor subtypes. |
University of Amsterdam |
22148859 |
190 |
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 |
22104008 |
64 |
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 |
22142423 |
27 |
Structure-activity relationships of truncated C2- or C8-substituted adenosine derivatives as dual acting A2A and A3 adenosine receptor ligands. |
Ewha Womans University |
22204739 |
136 |
Pyrrolo- and pyrazolo-[3,4-e][1,2,4]triazolo[1,5-c]pyrimidines as adenosine receptor antagonists. |
Universit£ |
21214204 |
100 |
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 |
21908194 |
88 |
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 |
21675777 |
139 |
New 2-heterocyclyl-imidazo[2,1-i]purin-5-one derivatives as potent and selective human A3 adenosine receptor antagonists. |
Universit£ |
21616671 |
13 |
Synthesis, structure-affinity relationships, and molecular modeling studies of novel pyrazolo[3,4-c]quinoline derivatives as adenosine receptor antagonists. |
Universita' Di Firenze |
21511471 |
83 |
Pharmacophore elucidation for a new series of 2-aryl-pyrazolo-triazolo-pyrimidines as potent human A3 adenosine receptor antagonists. |
National University of Singapore |
21185184 |
27 |
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 |
21401121 |
16 |
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 |
21388809 |
76 |
Discovery of benzothiazole-based adenosine A2B receptor antagonists with improved A2A selectivity. |
Roche Research Center |
24900298 |
100 |
Discovery of LAS101057: A Potent, Selective, and Orally Efficacious A2B Adenosine Receptor Antagonist |
TBA |
21186795 |
142 |
Pyrimidine derivatives as potent and selective A3 adenosine receptor antagonists. |
University of Santiago De Compostela |
20943397 |
18 |
Molecular modeling study on potent and selective adenosine A(3) receptor agonists. |
University of Camerino |
20937560 |
54 |
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 |
20801028 |
14 |
Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists. |
Niddk |
20728355 |
47 |
Identification and optimization of substituted 5-aminopyrazoles as potent and selective adenosine A1 receptor antagonists. |
Bayer Schering Pharma |
20826090 |
4 |
Design, synthesis, and binding of homologated truncated 4'-thioadenosine derivatives at the human A3 adenosine receptors. |
Ewha Womans University |
20813948 |
63 |
Spiroindolones, a potent compound class for the treatment of malaria. |
Swiss Tropical and Public Health Institute |
20591666 |
66 |
A new group of oxime carbamates as reversible inhibitors of fatty acid amide hydrolase. |
Università |
20537438 |
101 |
Insights into binding modes of adenosine A(2B) antagonists with ligand-based and receptor-based methods. |
East China University of Science and Technology |
20405927 |
13 |
Structure-based discovery of A2A adenosine receptor ligands. |
University of California |
20385496 |
66 |
Synthesis and evaluation of new N6-substituted adenosine-5'-N-methylcarboxamides as A3 adenosine receptor agonists. |
Monash University |
20307065 |
122 |
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 |
20304654 |
79 |
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 |
20138516 |
29 |
Discovery of potent and selective bicyclic A(2B) adenosine receptor antagonists via bioisosteric amide replacement. |
RhôNe-Poulenc Rorer |
20137946 |
81 |
Discovery of N-(5,6-diarylpyridin-2-yl)amide derivatives as potent and selective A(2B) adenosine receptor antagonists. |
RhôNe-Poulenc Rorer |
20036562 |
30 |
2-Dialkynyl derivatives of (N)-methanocarba nucleosides: 'Clickable' A(3) adenosine receptor-selective agonists. |
Niddk |
20031406 |
85 |
Synthesis and evaluation of two series of 4'-aza-carbocyclic nucleosides as adenosine A2A receptor agonists. |
Novartis Institutes For Biomedical Research |
20202853 |
12 |
Synthesis of theophylline derivatives and study of their activity as antagonists at adenosine receptors. |
Universidad De M£Laga |
19879151 |
58 |
Design and synthesis of N(6)-substituted-4'-thioadenosine-5'-uronamides as potent and selective human A(3) adenosine receptor agonists. |
Ewha Womans University |
19580286 |
44 |
Nucleoside-5'-monophosphates as prodrugs of adenosine A2A receptor agonists activated by ecto-5'-nucleotidase. |
University of Bonn |
19743865 |
22 |
2-Phenylpyrazolo[4,3-d]pyrimidin-7-one as a new scaffold to obtain potent and selective human A3 adenosine receptor antagonists: new insights into the receptor-antagonist recognition. |
Universit£ |
19499950 |
64 |
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 |
19839592 |
37 |
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 |
19501513 |
474 |
Combining selectivity and affinity predictions using an integrated Support Vector Machine (SVM) approach: An alternative tool to discriminate between the human adenosine A(2A) and A(3) receptor pyrazolo-triazolo-pyrimidine antagonists binding sites. |
Universit£ |
19481943 |
23 |
Synthesis of hybrid analogues of caffeine and eudistomin D and its affinity for adenosine receptors. |
Hokkaido University |
19375920 |
30 |
Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists. |
Ewha Womans University |
19362836 |
83 |
Antagonists of the human A(2A) receptor. Part 5: Highly bio-available pyrimidine-4-carboxamides. |
Vernalis (R+D) |
19161279 |
1 |
A series of 2,4-disubstituted quinolines as a new class of allosteric enhancers of the adenosine A3 receptor. |
Leiden University |
19398343 |
48 |
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 |
19317449 |
76 |
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 |
19301821 |
55 |
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 |
19284749 |
1 |
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 |
19230680 |
58 |
Synthesis, biological assays and QSAR studies of N-(9-benzyl-2-phenyl-8-azapurin-6-yl)-amides as ligands for A1 adenosine receptors. |
Università |
19140664 |
82 |
N-[6-amino-2-(heteroaryl)pyrimidin-4-yl]acetamides as A2A receptor antagonists with improved drug like properties and in vivo efficacy. |
Neurocrine Biosciences |
19072055 |
224 |
Antagonists of the human A(2A) adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-aryltriazolo[4,5-d]pyrimidines. |
Vernalis R&D |
19006671 |
136 |
Structure-activity relationship studies of a new series of imidazo[2,1-f]purinones as potent and selective A(3) adenosine receptor antagonists. |
Università |
18996701 |
38 |
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 |
18938084 |
78 |
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 |
18811138 |
41 |
Structure-activity relationships of truncated D- and l-4'-thioadenosine derivatives as species-independent A3 adenosine receptor antagonists. |
Ewha Womans University |
18809334 |
21 |
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 |
18752961 |
51 |
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 |
18588281 |
3 |
Ribose-modified purine nucleosides as ribonucleotide reductase inhibitors. Synthesis, antitumor activity, and molecular modeling of N6-substituted 3'-C-methyladenosine derivatives. |
Università |
18468446 |
55 |
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 |
18045744 |
16 |
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 |
17925440 |
2 |
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 |
18226896 |
129 |
Selective, high affinity A(2B) adenosine receptor antagonists: N-1 monosubstituted 8-(pyrazol-4-yl)xanthines. |
Cv Therapeutics |
18189346 |
21 |
Identification of novel, water-soluble, 2-amino-N-pyrimidin-4-yl acetamides as A2A receptor antagonists with in vivo efficacy. |
Neurocrine Biosciences |
18047262 |
13 |
Scouting human A3 adenosine receptor antagonist binding mode using a molecular simplification approach: from triazoloquinoxaline to a pyrimidine skeleton as a key study. |
Università |
17827019 |
86 |
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 |
17689079 |
36 |
Dual acting antioxidant A1 adenosine receptor agonists. |
Monash University (Parkville Campus) |
17665891 |
60 |
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 |
17560111 |
32 |
Design, synthesis, and biological evaluation of LNA nucleosides as adenosine A3 receptor ligands. |
Santaris Pharma |
17555308 |
30 |
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 |
17499511 |
46 |
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 |
17469811 |
45 |
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 |
17300165 |
39 |
2,6,8-trisubstituted 1-deazapurines as adenosine receptor antagonists. |
Leiden/Amsterdam Center For Drug Research |
17236762 |
23 |
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 |
17149867 |
51 |
2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists. |
Ghent University |
17125265 |
49 |
Tricyclic imidazoline derivatives as potent and selective adenosine A1 receptor antagonists. |
Biogen Idec |
17125264 |
60 |
Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists. |
Biogen Idec |
17045477 |
136 |
N6-Cycloalkyl-2-substituted adenosine derivatives as selective, high affinity adenosine A1 receptor agonists. |
Cv Therapeutics |
16821798 |
62 |
A new synthesis of sulfonamides by aminolysis of p-nitrophenylsulfonates yielding potent and selective adenosine A2B receptor antagonists. |
University of Bonn |
16821770 |
78 |
Pharmacophore based receptor modeling: the case of adenosine A3 receptor antagonists. An approach to the optimization of protein models. |
Università |
16789747 |
71 |
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 |
16759111 |
149 |
Novel 1,3-disubstituted 8-(1-benzyl-1H-pyrazol-4-yl) xanthines: high affinity and selective A2B adenosine receptor antagonists. |
Cv Therapeutics |
16722655 |
28 |
Discovery of a novel, orally active, small molecule gonadotropin-releasing hormone (GnRH) receptor antagonist. |
Pfizer |
16722654 |
15 |
Structure-activity relationships of new 1H-imidazo[4,5-c]quinolin-4-amine derivatives as allosteric enhancers of the A3 adenosine receptor. |
Leiden University |
16697192 |
59 |
New pyrrolopyrimidin-6-yl benzenesulfonamides: potent A2B adenosine receptor antagonists. |
RhôNe-Poulenc Rorer |
16686529 |
37 |
2,6-disubstituted and 2,6,8-trisubstituted purines as adenosine receptor antagonists. |
Leiden/Amsterdam Center For Drug Research |
16464581 |
21 |
The synthesis of highly potent, selective, and water-soluble agonists at the human adenosine A3 receptor. |
Pfizer |
16458504 |
37 |
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 |
16392812 |
75 |
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 |
16392798 |
46 |
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 |
16366590 |
12 |
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 |
16335918 |
68 |
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 |
16289820 |
14 |
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 |
16275090 |
136 |
Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists. |
Cv Therapeutics |
16033279 |
47 |
New 2-arylpyrazolo[4,3-c]quinoline derivatives as potent and selective human A3 adenosine receptor antagonists. |
Università |
16033270 |
44 |
"Reversine" and its 2-substituted adenine derivatives as potent and selective A3 adenosine receptor antagonists. |
National Institute of Diabetes and Digestive and Kidney Diseases |
16000006 |
59 |
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 |
15771421 |
96 |
(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 |
15664822 |
101 |
The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma. |
Cv Therapeutics |
15634009 |
123 |
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 |
15588088 |
58 |
2,4,6-trisubstituted pyrimidines as a new class of selective adenosine A1 receptor antagonists. |
Leiden/Amsterdam Center For Drug Research |
15294001 |
88 |
Piperazine derivatives of [1,2,4]triazolo[1,5-a][1,3,5]triazine as potent and selective adenosine A2a receptor antagonists. |
Biogen Idec |
15203160 |
124 |
Structure-activity relationships of adenosine A3 receptor ligands: new potential therapy for the treatment of glaucoma. |
Otsuka Pharmaceutical Factory |
15109629 |
19 |
Facile synthesis of fused 1,2,4-triazolo[1,5-c]pyrimidine derivatives as human adenosine A3 receptor ligands. |
Otsuka Pharmaceutical Factory |
15006389 |
33 |
2-(N-acyl) and 2-N-acyl-N(6)-substituted analogues of adenosine and their affinity at the human adenosine receptors. |
Inotek Pharmaceuticals |
14761205 |
56 |
Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability. |
University of Bonn |
13678407 |
57 |
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 |
12540233 |
16 |
3'-Aminoadenosine-5'-uronamides: discovery of the first highly selective agonist at the human adenosine A3 receptor. |
Pfizer |
12408713 |
54 |
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 |
12166943 |
81 |
1,2,4-Triazolo[5,1-i]purine derivatives as highly potent and selective human adenosine A(3) receptor ligands. |
Nutrition Research Institute |
12166930 |
21 |
Synthesis, biological properties, and molecular modeling investigation of the first potent, selective, and water-soluble human A(3) adenosine receptor antagonist. |
TBA |
12139445 |
36 |
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) |
12039562 |
17 |
2-Aminothiazoles: a new class of agonist allosteric enhancers of A(1) adenosine receptors. |
University of Virginia |
12014951 |
139 |
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 |
11906291 |
129 |
1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists. |
University of Bonn |
11831890 |
278 |
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 |
11754583 |
112 |
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 |
11527718 |
9 |
Synthesis and purine receptor affinity of 6-oxopurine nucleosides and nucleotides containing (N)-methanocarba-pseudoribose rings. |
Niddk |
32241719 |
68 |
New 8-amino-1,2,4-triazolo[4,3-a]pyrazin-3-one derivatives. Evaluation of different moieties on the 6-aryl ring to obtain potent and selective human A |
Universit£ |
32165041 |
52 |
Structural investigation on thiazolo[5,4-d]pyrimidines to obtain dual-acting blockers of CD73 and adenosine A |
Universit£ |
11495585 |
16 |
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 |
11454470 |
17 |
Substituted 4-phenyl-2-(phenylcarboxamido)-1,3-thiazole derivatives as antagonists for the adenosine A(1) receptor. |
Leiden/Amsterdam Center For Drug Research |
32573250 |
63 |
Nitrogen-Walk Approach to Explore Bioisosteric Replacements in a Series of Potent A |
Uppsala University |
11170626 |
55 |
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 |
11123985 |
176 |
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 |
11101355 |
26 |
7-Deazaadenines bearing polar substituents: structure-activity relationships of new A(1) and A(3) adenosine receptor antagonists. |
University of Leipzig |
11087559 |
7 |
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 |
30808606 |
240 |
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 |
10841801 |
33 |
Isoquinoline and quinazoline urea analogues as antagonists for the human adenosine A(3) receptor. |
Vrije Universiteit |
30576906 |
92 |
Novel non-xanthine antagonist of the A |
Bayer Pharmaceuticals |
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 |
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 |
10636237 |
10 |
The utilization of a unified pharmacophore query in the discovery of new antagonists of the adenosine receptor family. |
Chembridge |
31306001 |
117 |
Modifications on the Amino-3,5-dicyanopyridine Core To Obtain Multifaceted Adenosine Receptor Ligands with Antineuropathic Activity. |
Universit£ |
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 |
10514293 |
31 |
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 |
10447949 |
27 |
Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists. |
National Institute of Diabetes |
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 |
31990540 |
25 |
Synthesis of Novel Potent Archazolids: Pharmacology of an Emerging Class of Anticancer Drugs. |
Universit£T Bonn |
10052977 |
82 |
Synthesis, CoMFA analysis, and receptor docking of 3,5-diacyl-2, 4-dialkylpyridine derivatives as selective A3 adenosine receptor antagonists. |
National Institute of Diabetes |
31738058 |
154 |
Structure-Based Optimization of Coumarin hA |
University of Porto |
29939744 |
179 |
Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential. |
Shanghaitech University |
30605331 |
236 |
Design and in Vivo Characterization of A |
Medical College of Wisconsin |
9873431 |
18 |
The synthesis of new adenosine A3 selective ligands containing bioisosteric isoxazoles. |
Novo Nordisk |
9767637 |
31 |
A novel class of adenosine A3 receptor ligands. 2. Structure affinity profile of a series of isoquinoline and quinazoline compounds. |
Vrije Universiteit |
9767636 |
38 |
A novel class of adenosine A3 receptor ligands. 1. 3-(2-Pyridinyl)isoquinoline derivatives. |
Vrije Universiteit |
30835463 |
202 |
A |
Rheinische Friedrich-Wilhelms-Universitat Bonn |
9667972 |
119 |
Derivatives of the triazoloquinazoline adenosine antagonist (CGS 15943) having high potency at the human A2B and A3 receptor subtypes. |
National Institute of Diabetes |
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£ |
9258367 |
99 |
Structure-activity relationships of 4-(phenylethynyl)-6-phenyl-1,4-dihydropyridines as highly selective A3 adenosine receptor antagonists. |
National Institute of Diabetes |
31502843 |
2 |
Structural Characterization of Agonist Binding to an A |
National and Kapodistrian University of Athens |
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 |
8691424 |
61 |
Synthesis and biological activities of flavonoid derivatives as A3 adenosine receptor antagonists. |
National Institute of Diabetes |
8576921 |
63 |
Interactions of flavonoids and other phytochemicals with adenosine receptors. |
National Institute of Diabetes |
8558508 |
55 |
Tetrahydrobenzothiophenone derivatives as a novel class of adenosine receptor antagonists. |
National Institute of Diabetes |
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 |
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 |
24077183 |
32 |
Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives. |
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 |
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 |
15993066 |
17 |
QSAR of adenosine A3 receptor antagonist 1,2,4-triazolo[4,3-a]quinoxalin-1-one derivatives using chemometric tools. |
Jadavpur University |
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£ |
29718665 |
2 |
Emerging Approaches for the Identification of Protein Targets of Small Molecules - A Practitioners' Perspective. |
Abbvie |
29525433 |
41 |
The aminopyridine-3,5-dicarbonitrile core for the design of new non-nucleoside-like agonists of the human adenosine A |
Universit£ |
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 |
28528302 |
15 |
Nanomolar anti-sickling compounds identified by ligand-based pharmacophore approach. |
Universidade Estadual De Feira De Santana |
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 |
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 |
28368607 |
26 |
Enantiospecific Recognition at the A |
Uppsala University |
29446948 |
82 |
A Structure-Activity Relationship Study of Bitopic N |
Monash University |
28792759 |
22 |
Effect of Nitrogen Atom Substitution in A |
Uppsala University |
1654429 |
2 |
Synthesis and biological evaluation of 4-purinylpyrrolidine nucleosides. |
University of Minnesota |
29257884 |
75 |
Structure-Based Design, Synthesis, and In Vivo Antinociceptive Effects of Selective A |
University of Camerino |
28806076 |
60 |
Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine A |
Leiden University |
28799755 |
51 |
Polypharmacology of N |
Sahmyook University |
28238723 |
39 |
Non-steroidal Anti-inflammatory Drugs Are Caspase Inhibitors. |
University of Colorado |
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 |
26042529 |
21 |
Development of novel adenosine receptor ligands based on the 3-amidocoumarin scaffold. |
Universidade Do Porto |
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 |
19880322 |
56 |
N-acylpolyamine inhibitors of HDM2 and HDMX binding to p53. |
Nih |