A new series of 4-(1,3-dialkyl-2,4-dioxo-2,3,4,5-tetrahydro-1H-pyrrolo[3,2-d]pyrimidin-6-yl)benzenesulfonamides has been identified as potent A2B adenosine receptor antagonists. The products have been evaluated for their binding affinities for the human A2B, A1 and A3 adenosine receptors. 6-(4-{[4-(4-Bromobenzyl)piperazin-1-yl]sulfonyl}phenyl)-1,3-dimethyl-1H-pyrrolo[3,2-d]pyrimidine-2,4(3H,5H)-dione (16) showed a high affinity for the A2B adenosine receptor (IC50=1 nM) and selectivity (A1: 183x; A3: 12660x). Synthesis and SAR of this novel class of compounds showing improved absorption properties is presented herein.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/j.bmcl.2006.04.074 | DOI Listing |
Publication Analysis
Top Keywords
a2b adenosine
16
adenosine receptor
12
potent a2b
8
receptor antagonists
8
pyrrolopyrimidin-6-yl benzenesulfonamides
4
benzenesulfonamides potent
4
a2b
4
adenosine
4
antagonists series
4
series 4-13-dialkyl-24-dioxo-2345-tetrahydro-1h-pyrrolo[32-d]pyrimidin-6-ylbenzenesulfonamides
4
Similar Publications
Want AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!