612095-46-2Relevant academic research and scientific papers
New pyrrolopyrimidin-6-yl benzenesulfonamides: Potent A2B adenosine receptor antagonists
Esteve, Cristina,Nueda, Arsenio,Diaz, Jose Luis,Beleta, Jorge,Cardenas, Alvaro,Lozoya, Estrella,Cadavid, Maria Isabel,Loza, Maria Isabel,Ryder, Hamish,Vidal, Bernat
, p. 3642 - 3645 (2008/09/21)
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.
NEW-4-(PYRROLOPYRIMIDIN-6-YL)BENZENESULPHONAMIDE DERIVATIVES
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Page/Page column 33-34, (2008/06/13)
This invention is directed to new potent and selective antagonists of A2A and/or A2B adenosine receptors having the general formula (I) to process for their preparation; to pharmaceutical compositions comprising them; and to their us
