New pyrrolopyrimidin-6-yl benzenesulfonamides: potent A2B adenosine receptor antagonists |
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Authors: | Esteve Cristina Nueda Arsenio Díaz José Luis Beleta Jorge Cárdenas Alvaro Lozoya Estrella Cadavid Maria Isabel Loza Maria Isabel Ryder Hamish Vidal Bernat |
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Institution: | Medicinal Chemistry Department, Almirall, Treball 2-4, E-08960 St. Just Desvern, Barcelona, Spain. |
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Abstract: | A new series of 4-(1,3-dialkyl-2,4-dioxo-2,3,4,5-tetrahydro-1H-pyrrolo3,2-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-pyrrolo3,2-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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