Pyrazolo-triazolo-pyrimidines as adenosine receptor antagonists: A complete structure-activity profile

Purinergic Signalling

Volumn 3, Issue 3, 2007, Pages 183-193

  Cacciari, Barbara ^a   Bolcato, Chiara ^b   Spalluto, Giampiero ^b   Klotz, Karl Norbet ^c   Bacilieri, Magdalena ^d   Deflorian, Francesca ^d   Moro, Stefano ^d  

^a UNIVERSITY OF FERRARA   (Italy)

^b UNIVERSITY OF TRIESTE   (Italy)

^c UNIVERSITY OF WÜRZBURG   (Germany)

^d UNIVERSITY OF PADOVA   (Italy)

Author keywords

Adenosine receptors; Antagonists; Binding; Molecular modeling; Pyrazolo triazolo pyrimidines

Indexed keywords

EID: 34249912374     PISSN: 15739538     EISSN: 15739546     Source Type: Journal    
DOI: 10.1007/s11302-006-9027-x     Document Type: Review

References (30)

1. 3 Adenosine receptor ligands; history and perspectives. Med Res Rev 20:103-128
2. Baraldi PG, Cacciari B, Borea PA, Varani K, Pastorin G, Da Ros T, Tabrizi MA, Fruttarolo F, Spalluto G (2002) Pyrazolo-triazolo-pyrimidines as adenosine receptor antagonists: A possible template for adenosine receptor subtypes? Curr Pharm Des 8:2299-2332
3. 2 adenosine receptor antagonist 8FB-PTP, an 8 substituted pyrazolo-triazolo-pyrimidine, on in vitro functional models. Br J Pharmacol 112: 659-665
4. 9 adenosine receptor antagonists. Bioorg Med Chem Lett 4:2539-2544
5. 2A adenosine antagonists. J Med Chem 39:1164-1171
6. 2A adenosine receptor antagonists. J Med Chem 41:2126-2133
7. 2A receptor system using positron emission tomography. J Med Chem 43:4359-4362
8. 2A adenosine receptor antagonists: A study on the importance of modifications at the side chain on the activity and solubility. J Med Chem 45:115-126
9. 3 receptor subtype. J Med Chem 39:4142-4148
10. 3 adenosine receptors. J Med Chem 39:802-806
11. 3 adenosine receptor antagonists. J Med Chem 41:3174-3185
12. 3 adenosine receptor antagonists. J Med Chem 42:4473-4478
13. 8 pyrazole nitrogen. J Med Chem 43:4768-4780
14. 3 adenosine receptors. Bioorg Med Chem Lett 10:209-211
15. 3 adenosine receptors. Mol Pharmacol 57:968-975
16. 3 adenosine receptor antagonists. J Med Chem 45:770-780
17. 3 adenosine receptor antagonist. J Med Chem 45:3579-3582
18. 3 receptor subtypes. J Med Chem 41:2835-2845
19. 2B adenosine receptor antagonists. Drug Dev Res 53:225-235
20. 2B adenosine receptor subtypes: A molecular modeling investigation. J Med Chem 46:4287-4296
21. Moro S, Deflorian F, Spalluto G, Pastorin G, Cacciari B, Kim SK, Jacobson KA (2003) Demystifying the three-dimensional structure of G preotein-coupled receptors (GPCRs) with the aid of molecular modeling. Chem Commun (Cambridge) 21(24):2949-2956
22. 3 adenosine receptor antagonists: Pyrazolo[4,3- e] 1,2,4-triazolo[1,5- c] pyrimidine derivatives as a key study. J Med Chem 48:152-162
23. Moro S, Bacilieri M, Deflorian F, Spalluto G (2006) G protein-coupled receptors as challenging druggable targets: Insights from in silico studies. New J Chem 30:301-308
24. Moro S, Bacilieri M, Deflorian F, Spalluto G (2006) Ligand-based homology modeling as attractive tool to inspect GPCR structural plasticity. Curr Pharm Des 12:2175-2185
25. Palczewski K, Kumasaka T, Hori T, Behnke CA, Motoshima H, Fox BA, Le Trong I, Teller DC, Okada T, Stenkamp RE, Yamamoto M, Miyano M (2000) Crystal structure of rhodopsine: A G protein couplet receptor. Science 289:739-745
26. 3 receptor antagonists: An update. Curr Med Chem 13:639-645
27. 3 adenosine receptor. J Biol Chem 277:19056-19063
28. 2a adenosine receptors and biogenic amine G protein-coupled receptors. J Med Chem 40:2588-2595
29. 3 adenosine receptor antagonists. Influence of the heteroaryl substituent on binding affinity and molecular modeling investigation. J Med Chem 49:1720-1729
30. 3 adenosine receptor antagonists. J Med Chem 46:1229-1241