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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.
| Content Provider | Semantic Scholar |
|---|---|
| Author | Baraldi, Pier Giovanni Preti, Delia Tabrizi, Mojgan Aghazadeh Fruttarolo, Francesca Romagnoli, Romeo Zaid, Naser Abdel Moorman, Allan R. Merighi, Stefania Varani, Katia Borea, Pier Andrea |
| Copyright Year | 2005 |
| Abstract | Compounds presenting an additional fused ring on the xanthine nucleus have been reported to exhibit antagonistic activity with various levels of affinity and selectivity toward the four adenosine receptors subtypes A(1), A(2A), A(2B), and A(3). This paper reports synthesis and biological evaluation of new 1-benzyl-3-propyl-1H,6H-pyrrolo[2,1-f]purine-2,4-diones and 1-benzyl-3-propyl-1H,8H-imidazo[2,1-f]purine-2,4-diones, among which we identified potent and selective A(3) adenosine receptors antagonists. In particular, 1-benzyl-7-methyl-3-propyl-1H,8H-imidazo[2,1-f]purine-2,4-dione (11e) shows a K(i) (hA(3)) value from binding assay of 0.8 nM. |
| File Format | PDF HTM / HTML |
| DOI | 10.1021/jm058008c |
| Alternate Webpage(s) | http://blogs.najah.edu/staff/emp_2384/article/New-Pyrrolo21-fpurine-24-dione-and-Imidazo21-fpurine-24-dione-Derivatives-as-Potent-and-Selective-Human-A3-Adenosine-Receptor-Antagonists/file/JEMED-CHEM-2.pdf |
| PubMed reference number | 16000006 |
| Alternate Webpage(s) | https://doi.org/10.1021/jm058008c |
| Journal | Medline |
| Volume Number | 48 |
| Issue Number | 14 |
| Journal | Journal of medicinal chemistry |
| Language | English |
| Access Restriction | Open |
| Content Type | Text |
| Resource Type | Article |
