Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377918 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
Abstract
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.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Cristina Esteve, Arsenio Nueda, José Luis Díaz, Jorge Beleta, Alvaro Cárdenas, Estrella Lozoya, Maria Isabel Cadavid, Maria Isabel Loza, Hamish Ryder, Bernat Vidal,